Design, Synthesis, Antimicrobial, and Anticancer Activities of Acridine Thiosemicarbazides Derivatives
Identifieur interne : 000714 ( Pmc/Curation ); précédent : 000713; suivant : 000715Design, Synthesis, Antimicrobial, and Anticancer Activities of Acridine Thiosemicarbazides Derivatives
Auteurs : Rui Chen [République populaire de Chine] ; Lini Huo ; Yogini Jaiswal ; Jiayong Huang ; Zhenguo Zhong ; Jing Zhong ; Leonard Williams ; Xing Xia ; Yan Liang ; Zhenshuo YanSource :
- Molecules [ 1420-3049 ] ; 2019.
Abstract
Url:
DOI: 10.3390/molecules24112065
PubMed: 31151235
PubMed Central: 6600397
Links toward previous steps (curation, corpus...)
- to stream Pmc, to step Corpus: Pour aller vers cette notice dans l'étape Curation :000714
Links to Exploration step
PMC:6600397Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Design, Synthesis, Antimicrobial, and Anticancer Activities of Acridine Thiosemicarbazides Derivatives</title>
<author><name sortKey="Chen, Rui" sort="Chen, Rui" uniqKey="Chen R" first="Rui" last="Chen">Rui Chen</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
<affiliation wicri:level="1"><nlm:aff id="af2-molecules-24-02065">Faculty of Chinese Medicine Science, Guangxi University of Chinese Medicine, Nanning 530222, China</nlm:aff>
<country xml:lang="fr">République populaire de Chine</country>
<wicri:regionArea>Faculty of Chinese Medicine Science, Guangxi University of Chinese Medicine, Nanning 530222</wicri:regionArea>
</affiliation>
</author>
<author><name sortKey="Huo, Lini" sort="Huo, Lini" uniqKey="Huo L" first="Lini" last="Huo">Lini Huo</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Jaiswal, Yogini" sort="Jaiswal, Yogini" uniqKey="Jaiswal Y" first="Yogini" last="Jaiswal">Yogini Jaiswal</name>
<affiliation><nlm:aff id="af3-molecules-24-02065">Center for Excellence in Post-Harvest Technologies, North Carolina A&T State University, The North Carolina Research Campus, 500 Laureate Way, Kannapolis, NC-28081, USA;<email>yoginijaiswal@gmail.com</email>
(Y.J.);<email>llw@ncat.edu</email>
(L.W.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Huang, Jiayong" sort="Huang, Jiayong" uniqKey="Huang J" first="Jiayong" last="Huang">Jiayong Huang</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Zhong, Zhenguo" sort="Zhong, Zhenguo" uniqKey="Zhong Z" first="Zhenguo" last="Zhong">Zhenguo Zhong</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Zhong, Jing" sort="Zhong, Jing" uniqKey="Zhong J" first="Jing" last="Zhong">Jing Zhong</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Williams, Leonard" sort="Williams, Leonard" uniqKey="Williams L" first="Leonard" last="Williams">Leonard Williams</name>
<affiliation><nlm:aff id="af3-molecules-24-02065">Center for Excellence in Post-Harvest Technologies, North Carolina A&T State University, The North Carolina Research Campus, 500 Laureate Way, Kannapolis, NC-28081, USA;<email>yoginijaiswal@gmail.com</email>
(Y.J.);<email>llw@ncat.edu</email>
(L.W.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Xia, Xing" sort="Xia, Xing" uniqKey="Xia X" first="Xing" last="Xia">Xing Xia</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Liang, Yan" sort="Liang, Yan" uniqKey="Liang Y" first="Yan" last="Liang">Yan Liang</name>
<affiliation><nlm:aff id="af4-molecules-24-02065">College of Pharmacy, Guangxi Medical University, Nanning 530021, China;<email>vincyliang@163.com</email>
</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Yan, Zhenshuo" sort="Yan, Zhenshuo" uniqKey="Yan Z" first="Zhenshuo" last="Yan">Zhenshuo Yan</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
</author>
</titleStmt>
<publicationStmt><idno type="wicri:source">PMC</idno>
<idno type="pmid">31151235</idno>
<idno type="pmc">6600397</idno>
<idno type="url">http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6600397</idno>
<idno type="RBID">PMC:6600397</idno>
<idno type="doi">10.3390/molecules24112065</idno>
<date when="2019">2019</date>
<idno type="wicri:Area/Pmc/Corpus">000714</idno>
<idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Corpus" wicri:corpus="PMC">000714</idno>
<idno type="wicri:Area/Pmc/Curation">000714</idno>
<idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Curation">000714</idno>
</publicationStmt>
<sourceDesc><biblStruct><analytic><title xml:lang="en" level="a" type="main">Design, Synthesis, Antimicrobial, and Anticancer Activities of Acridine Thiosemicarbazides Derivatives</title>
<author><name sortKey="Chen, Rui" sort="Chen, Rui" uniqKey="Chen R" first="Rui" last="Chen">Rui Chen</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
<affiliation wicri:level="1"><nlm:aff id="af2-molecules-24-02065">Faculty of Chinese Medicine Science, Guangxi University of Chinese Medicine, Nanning 530222, China</nlm:aff>
<country xml:lang="fr">République populaire de Chine</country>
<wicri:regionArea>Faculty of Chinese Medicine Science, Guangxi University of Chinese Medicine, Nanning 530222</wicri:regionArea>
</affiliation>
</author>
<author><name sortKey="Huo, Lini" sort="Huo, Lini" uniqKey="Huo L" first="Lini" last="Huo">Lini Huo</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Jaiswal, Yogini" sort="Jaiswal, Yogini" uniqKey="Jaiswal Y" first="Yogini" last="Jaiswal">Yogini Jaiswal</name>
<affiliation><nlm:aff id="af3-molecules-24-02065">Center for Excellence in Post-Harvest Technologies, North Carolina A&T State University, The North Carolina Research Campus, 500 Laureate Way, Kannapolis, NC-28081, USA;<email>yoginijaiswal@gmail.com</email>
(Y.J.);<email>llw@ncat.edu</email>
(L.W.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Huang, Jiayong" sort="Huang, Jiayong" uniqKey="Huang J" first="Jiayong" last="Huang">Jiayong Huang</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Zhong, Zhenguo" sort="Zhong, Zhenguo" uniqKey="Zhong Z" first="Zhenguo" last="Zhong">Zhenguo Zhong</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Zhong, Jing" sort="Zhong, Jing" uniqKey="Zhong J" first="Jing" last="Zhong">Jing Zhong</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Williams, Leonard" sort="Williams, Leonard" uniqKey="Williams L" first="Leonard" last="Williams">Leonard Williams</name>
<affiliation><nlm:aff id="af3-molecules-24-02065">Center for Excellence in Post-Harvest Technologies, North Carolina A&T State University, The North Carolina Research Campus, 500 Laureate Way, Kannapolis, NC-28081, USA;<email>yoginijaiswal@gmail.com</email>
(Y.J.);<email>llw@ncat.edu</email>
(L.W.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Xia, Xing" sort="Xia, Xing" uniqKey="Xia X" first="Xing" last="Xia">Xing Xia</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Liang, Yan" sort="Liang, Yan" uniqKey="Liang Y" first="Yan" last="Liang">Yan Liang</name>
<affiliation><nlm:aff id="af4-molecules-24-02065">College of Pharmacy, Guangxi Medical University, Nanning 530021, China;<email>vincyliang@163.com</email>
</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Yan, Zhenshuo" sort="Yan, Zhenshuo" uniqKey="Yan Z" first="Zhenshuo" last="Yan">Zhenshuo Yan</name>
<affiliation><nlm:aff id="af1-molecules-24-02065">College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</nlm:aff>
</affiliation>
</author>
</analytic>
<series><title level="j">Molecules</title>
<idno type="eISSN">1420-3049</idno>
<imprint><date when="2019">2019</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
</fileDesc>
<profileDesc><textClass></textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en"><p><bold>Background:</bold>
Acridine and thiourea derivatives are important compounds in medicinal chemistry due to their diverse biological properties including anticancer and antimicrobial effects. However, literature reveals some side effects associated with use of acridines. It is suggested that hybrid molecules may reduce the side effects and enhance the beneficial properties due to synergistic activity. The objectives of the present study are to synthesize and evaluate the anticancer and antimicrobial properties of new hybrids of acridine thiosemicarbazides derivatives. <bold>Results:</bold>
The structures of the synthesized compounds <bold>4a–4e</bold>
were elucidated by MS and NMR spectra. In antimicrobial assay, Compound <bold>4c</bold>
exhibited potent antimicrobial activity compared to the other four compounds. In anticancer studies, we observed that compounds <bold>4a</bold>
, <bold>4b</bold>
, <bold>4d</bold>
and <bold>4e</bold>
exhibited high cytotoxicity against the MT-4 cell line, with IC50 values of 18.42 ± 1.18, 15.73 ± 0.90, 10.96 ± 0.62 and 11.63 ± 0.11 μM, respectively. The evaluation of anticancer effects, and the associated mechanism reveals that, the anticancer activities may be related to Topo I inhibitory activity, apoptosis and cell-cycle. Molecular docking studies revealed that the presence of planar naphtho-fused rings and a flexible thiourea group together, could improve DNA-intercalation and inhibition of DNA-Topo I activity. <bold>Conclusions:</bold>
The results of this study demonstrate that the rational design of target derivatives as novel antimicrobial or antitumor leads is feasible.</p>
</div>
</front>
<back><div1 type="bibliography"><listBibl><biblStruct><analytic><author><name sortKey="Lang, X" uniqKey="Lang X">X. Lang</name>
</author>
<author><name sortKey="Luan, X" uniqKey="Luan X">X. Luan</name>
</author>
<author><name sortKey="Gao, C" uniqKey="Gao C">C. Gao</name>
</author>
<author><name sortKey="Jiang, Y" uniqKey="Jiang Y">Y. Jiang</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Wang, S S" uniqKey="Wang S">S.S. Wang</name>
</author>
<author><name sortKey="Lee, Y J" uniqKey="Lee Y">Y.J. Lee</name>
</author>
<author><name sortKey="Hsu, S C" uniqKey="Hsu S">S.C. Hsu</name>
</author>
<author><name sortKey="Chang, H O" uniqKey="Chang H">H.O. Chang</name>
</author>
<author><name sortKey="Yin, W K" uniqKey="Yin W">W.K. Yin</name>
</author>
<author><name sortKey="Chang, L S" uniqKey="Chang L">L.S. Chang</name>
</author>
<author><name sortKey="Chou, S Y" uniqKey="Chou S">S.Y. Chou</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Sanchez, I" uniqKey="Sanchez I">I. Sánchez</name>
</author>
<author><name sortKey="Reches, R" uniqKey="Reches R">R. Reches</name>
</author>
<author><name sortKey="Caignard, D H" uniqKey="Caignard D">D.H. Caignard</name>
</author>
<author><name sortKey="Renard, P" uniqKey="Renard P">P. Renard</name>
</author>
<author><name sortKey="Pujol, M D" uniqKey="Pujol M">M.D. Pujol</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Bacherikov, V A" uniqKey="Bacherikov V">V.A. Bacherikov</name>
</author>
<author><name sortKey="Chang, J Y" uniqKey="Chang J">J.Y. Chang</name>
</author>
<author><name sortKey="Lin, Y W" uniqKey="Lin Y">Y.W. Lin</name>
</author>
<author><name sortKey="Chen, C H" uniqKey="Chen C">C.H. Chen</name>
</author>
<author><name sortKey="Pan, W Y" uniqKey="Pan W">W.Y. Pan</name>
</author>
<author><name sortKey="Dong, H" uniqKey="Dong H">H. Dong</name>
</author>
<author><name sortKey="Lee, R Z" uniqKey="Lee R">R.Z. Lee</name>
</author>
<author><name sortKey="Chou, T C" uniqKey="Chou T">T.C. Chou</name>
</author>
<author><name sortKey="Su, T L" uniqKey="Su T">T.L. Su</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Vispe, S" uniqKey="Vispe S">S. Vispé</name>
</author>
<author><name sortKey="Vandenberghe, I" uniqKey="Vandenberghe I">I. Vandenberghe</name>
</author>
<author><name sortKey="Robin, M" uniqKey="Robin M">M. Robin</name>
</author>
<author><name sortKey="Annereau, J P" uniqKey="Annereau J">J.P. Annereau</name>
</author>
<author><name sortKey="Creancier, L" uniqKey="Creancier L">L. Créancier</name>
</author>
<author><name sortKey="Pique, V" uniqKey="Pique V">V. Pique</name>
</author>
<author><name sortKey="Galy, J P" uniqKey="Galy J">J.P. Galy</name>
</author>
<author><name sortKey="Kruczynski, A" uniqKey="Kruczynski A">A. Kruczynski</name>
</author>
<author><name sortKey="Barret, J M" uniqKey="Barret J">J.M. Barret</name>
</author>
<author><name sortKey="Bailly, C" uniqKey="Bailly C">C. Bailly</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Belmont, P" uniqKey="Belmont P">P. Belmont</name>
</author>
<author><name sortKey="Bosson, J" uniqKey="Bosson J">J. Bosson</name>
</author>
<author><name sortKey="Godet, T" uniqKey="Godet T">T. Godet</name>
</author>
<author><name sortKey="Tiano, M" uniqKey="Tiano M">M. Tiano</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Oppegard, L M" uniqKey="Oppegard L">L.M. Oppegard</name>
</author>
<author><name sortKey="Ougolkov, A V" uniqKey="Ougolkov A">A.V. Ougolkov</name>
</author>
<author><name sortKey="Luchini, D N" uniqKey="Luchini D">D.N. Luchini</name>
</author>
<author><name sortKey="Schoon, R A" uniqKey="Schoon R">R.A. Schoon</name>
</author>
<author><name sortKey="Goodell, J R" uniqKey="Goodell J">J.R. Goodell</name>
</author>
<author><name sortKey="Kaur, H" uniqKey="Kaur H">H. Kaur</name>
</author>
<author><name sortKey="Billadeau, D D" uniqKey="Billadeau D">D.D. Billadeau</name>
</author>
<author><name sortKey="Ferguson, D M" uniqKey="Ferguson D">D.M. Ferguson</name>
</author>
<author><name sortKey="Hiasaa, H" uniqKey="Hiasaa H">H. Hiasaa</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Cain, B F" uniqKey="Cain B">B.F. Cain</name>
</author>
<author><name sortKey="Atwell, G J" uniqKey="Atwell G">G.J. Atwell</name>
</author>
<author><name sortKey="Denny, W A" uniqKey="Denny W">W.A. Denny</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Kimura, M" uniqKey="Kimura M">M. Kimura</name>
</author>
<author><name sortKey="Okabayashi, I" uniqKey="Okabayashi I">I. Okabayashi</name>
</author>
<author><name sortKey="Kato, A" uniqKey="Kato A">A. Kato</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Gamage, S A" uniqKey="Gamage S">S.A. Gamage</name>
</author>
<author><name sortKey="Spicer, J A" uniqKey="Spicer J">J.A. Spicer</name>
</author>
<author><name sortKey="Rewcastle, G W" uniqKey="Rewcastle G">G.W. Rewcastle</name>
</author>
<author><name sortKey="Denny, W A" uniqKey="Denny W">W.A. Denny</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Abbas, S Y" uniqKey="Abbas S">S.Y. Abbas</name>
</author>
<author><name sortKey="Elsharief, M A" uniqKey="Elsharief M">M.A. Elsharief</name>
</author>
<author><name sortKey="Basyouni, W M" uniqKey="Basyouni W">W.M. Basyouni</name>
</author>
<author><name sortKey="Fakhr, I M" uniqKey="Fakhr I">I.M. Fakhr</name>
</author>
<author><name sortKey="Elgammal, E W" uniqKey="Elgammal E">E.W. Elgammal</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Saeed, S" uniqKey="Saeed S">S. Saeed</name>
</author>
<author><name sortKey="Rashid, N" uniqKey="Rashid N">N. Rashid</name>
</author>
<author><name sortKey="Jones, P G" uniqKey="Jones P">P.G. Jones</name>
</author>
<author><name sortKey="Ali, M" uniqKey="Ali M">M. Ali</name>
</author>
<author><name sortKey="Hussain, R" uniqKey="Hussain R">R. Hussain</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Zhong, Z" uniqKey="Zhong Z">Z. Zhong</name>
</author>
<author><name sortKey="Xing, R" uniqKey="Xing R">R. Xing</name>
</author>
<author><name sortKey="Liu, S" uniqKey="Liu S">S. Liu</name>
</author>
<author><name sortKey="Wang, L" uniqKey="Wang L">L. Wang</name>
</author>
<author><name sortKey="Cai, S" uniqKey="Cai S">S. Cai</name>
</author>
<author><name sortKey="Li, P" uniqKey="Li P">P. Li</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Rao, X P" uniqKey="Rao X">X.P. Rao</name>
</author>
<author><name sortKey="Wu, Y" uniqKey="Wu Y">Y. Wu</name>
</author>
<author><name sortKey="Song, Z Q" uniqKey="Song Z">Z.Q. Song</name>
</author>
<author><name sortKey="Shang, S B" uniqKey="Shang S">S.B. Shang</name>
</author>
<author><name sortKey="Wang, Z D" uniqKey="Wang Z">Z.D. Wang</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Burgeson, J R" uniqKey="Burgeson J">J.R. Burgeson</name>
</author>
<author><name sortKey="Moore, A L" uniqKey="Moore A">A.L. Moore</name>
</author>
<author><name sortKey="Boutilier, J K" uniqKey="Boutilier J">J.K. Boutilier</name>
</author>
<author><name sortKey="Cerruti, N R" uniqKey="Cerruti N">N.R. Cerruti</name>
</author>
<author><name sortKey="Gharaibeh, D N" uniqKey="Gharaibeh D">D.N. Gharaibeh</name>
</author>
<author><name sortKey="Lovejoy, C E" uniqKey="Lovejoy C">C.E. Lovejoy</name>
</author>
<author><name sortKey="Amberg, S M" uniqKey="Amberg S">S.M. Amberg</name>
</author>
<author><name sortKey="Hruby, D E" uniqKey="Hruby D">D.E. Hruby</name>
</author>
<author><name sortKey="Tyavanagimatt, S R" uniqKey="Tyavanagimatt S">S.R. Tyavanagimatt</name>
</author>
<author><name sortKey="Alleniii, R D" uniqKey="Alleniii R">R.D. AllenIII</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Limban, C" uniqKey="Limban C">C. Limban</name>
</author>
<author><name sortKey="Vasile, A" uniqKey="Vasile A">A. Vasile</name>
</author>
<author><name sortKey="Chirita, I C" uniqKey="Chirita I">I.C. Chirita</name>
</author>
<author><name sortKey="Caproiu, M" uniqKey="Caproiu M">M. Caproiu</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Burgess, S J" uniqKey="Burgess S">S.J. Burgess</name>
</author>
<author><name sortKey="Audrey, S" uniqKey="Audrey S">S. Audrey</name>
</author>
<author><name sortKey="Jane Xu, K" uniqKey="Jane Xu K">K. Jane Xu</name>
</author>
<author><name sortKey="Smilkstein, M J" uniqKey="Smilkstein M">M.J. Smilkstein</name>
</author>
<author><name sortKey="Riscoe, M K" uniqKey="Riscoe M">M.K. Riscoe</name>
</author>
<author><name sortKey="Peyton, D H" uniqKey="Peyton D">D.H. Peyton</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Solinas, A" uniqKey="Solinas A">A. Solinas</name>
</author>
<author><name sortKey="Faure, H" uniqKey="Faure H">H. Faure</name>
</author>
<author><name sortKey="Roudaut, H" uniqKey="Roudaut H">H. Roudaut</name>
</author>
<author><name sortKey="Traiffort, E" uniqKey="Traiffort E">E. Traiffort</name>
</author>
<author><name sortKey="Schoenfelder, A" uniqKey="Schoenfelder A">A. Schoenfelder</name>
</author>
<author><name sortKey="Mann, A" uniqKey="Mann A">A. Mann</name>
</author>
<author><name sortKey="Manetti, F" uniqKey="Manetti F">F. Manetti</name>
</author>
<author><name sortKey="Taddei, M" uniqKey="Taddei M">M. Taddei</name>
</author>
<author><name sortKey="Ruat, M" uniqKey="Ruat M">M. Ruat</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Pommier, Y" uniqKey="Pommier Y">Y. Pommier</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Zhao, L X" uniqKey="Zhao L">L.X. Zhao</name>
</author>
<author><name sortKey="Moon, Y S" uniqKey="Moon Y">Y.S. Moon</name>
</author>
<author><name sortKey="Basnet, A" uniqKey="Basnet A">A. Basnet</name>
</author>
<author><name sortKey="Kim, E K" uniqKey="Kim E">E.K. Kim</name>
</author>
<author><name sortKey="Jahng, Y" uniqKey="Jahng Y">Y. Jahng</name>
</author>
<author><name sortKey="Park, J G" uniqKey="Park J">J.G. Park</name>
</author>
<author><name sortKey="Jeong, T C" uniqKey="Jeong T">T.C. Jeong</name>
</author>
<author><name sortKey="Cho, W J" uniqKey="Cho W">W.J. Cho</name>
</author>
<author><name sortKey="Choi, S U" uniqKey="Choi S">S.U. Choi</name>
</author>
<author><name sortKey="Chong, O L" uniqKey="Chong O">O.L. Chong</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Lill, M" uniqKey="Lill M">M. Lill</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Hevener, K E" uniqKey="Hevener K">K.E. Hevener</name>
</author>
<author><name sortKey="Zhao, W" uniqKey="Zhao W">W. Zhao</name>
</author>
<author><name sortKey="Ball, D M" uniqKey="Ball D">D.M. Ball</name>
</author>
<author><name sortKey="Babaoglu, K" uniqKey="Babaoglu K">K. Babaoglu</name>
</author>
<author><name sortKey="Qi, J" uniqKey="Qi J">J. Qi</name>
</author>
<author><name sortKey="White, S W" uniqKey="White S">S.W. White</name>
</author>
<author><name sortKey="Lee, R E" uniqKey="Lee R">R.E. Lee</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Maddika, S" uniqKey="Maddika S">S. Maddika</name>
</author>
<author><name sortKey="Raoande, S" uniqKey="Raoande S">S. RaoAnde</name>
</author>
<author><name sortKey="Panigrahi, S" uniqKey="Panigrahi S">S. Panigrahi</name>
</author>
<author><name sortKey="Paranjothy, T" uniqKey="Paranjothy T">T. Paranjothy</name>
</author>
<author><name sortKey="Weglarczyk, K" uniqKey="Weglarczyk K">K. Weglarczyk</name>
</author>
<author><name sortKey="Zuse, A" uniqKey="Zuse A">A. Zuse</name>
</author>
<author><name sortKey="Eshraghi, M" uniqKey="Eshraghi M">M. Eshraghi</name>
</author>
<author><name sortKey="Manda, K D" uniqKey="Manda K">K.D. Manda</name>
</author>
<author><name sortKey="Wiechec, E" uniqKey="Wiechec E">E. Wiechec</name>
</author>
<author><name sortKey="Los, M" uniqKey="Los M">M. Los</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Bunz, F" uniqKey="Bunz F">F. Bunz</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Liu, K" uniqKey="Liu K">K. Liu</name>
</author>
<author><name sortKey="Liu, P" uniqKey="Liu P">P. Liu</name>
</author>
<author><name sortKey="Liu, R" uniqKey="Liu R">R. Liu</name>
</author>
<author><name sortKey="Wu, X" uniqKey="Wu X">X. Wu</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Huang, X C" uniqKey="Huang X">X.C. Huang</name>
</author>
<author><name sortKey="Wang, M" uniqKey="Wang M">M. Wang</name>
</author>
<author><name sortKey="Wang, H S" uniqKey="Wang H">H.S. Wang</name>
</author>
<author><name sortKey="Chen, Z F" uniqKey="Chen Z">Z.F. Chen</name>
</author>
<author><name sortKey="Zhang, Y" uniqKey="Zhang Y">Y. Zhang</name>
</author>
<author><name sortKey="Pan, Y M" uniqKey="Pan Y">Y.M. Pan</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Cappuccino, J" uniqKey="Cappuccino J">J. Cappuccino</name>
</author>
<author><name sortKey="Sherman, N" uniqKey="Sherman N">N. Sherman</name>
</author>
</analytic>
</biblStruct>
<biblStruct></biblStruct>
<biblStruct><analytic><author><name sortKey="Jin, Y" uniqKey="Jin Y">Y. Jin</name>
</author>
<author><name sortKey="Chen, Q" uniqKey="Chen Q">Q. Chen</name>
</author>
<author><name sortKey="Shi, X" uniqKey="Shi X">X. Shi</name>
</author>
<author><name sortKey="Lu, Z" uniqKey="Lu Z">Z. Lu</name>
</author>
<author><name sortKey="Cheng, C" uniqKey="Cheng C">C. Cheng</name>
</author>
<author><name sortKey="Lai, Y" uniqKey="Lai Y">Y. Lai</name>
</author>
<author><name sortKey="Zheng, Q" uniqKey="Zheng Q">Q. Zheng</name>
</author>
<author><name sortKey="Pan, J" uniqKey="Pan J">J. Pan</name>
</author>
</analytic>
</biblStruct>
<biblStruct><analytic><author><name sortKey="Xu, Y" uniqKey="Xu Y">Y. Xu</name>
</author>
<author><name sortKey="Jing, D" uniqKey="Jing D">D. Jing</name>
</author>
<author><name sortKey="Chen, R" uniqKey="Chen R">R. Chen</name>
</author>
<author><name sortKey="Haroon, U R" uniqKey="Haroon U">U.R. Haroon</name>
</author>
<author><name sortKey="Jiang, J" uniqKey="Jiang J">J. Jiang</name>
</author>
<author><name sortKey="Liu, X" uniqKey="Liu X">X. Liu</name>
</author>
<author><name sortKey="Wang, L" uniqKey="Wang L">L. Wang</name>
</author>
<author><name sortKey="Wang, P" uniqKey="Wang P">P. Wang</name>
</author>
</analytic>
</biblStruct>
</listBibl>
</div1>
</back>
</TEI>
<pmc article-type="research-article"><pmc-dir>properties open_access</pmc-dir>
<front><journal-meta><journal-id journal-id-type="nlm-ta">Molecules</journal-id>
<journal-id journal-id-type="iso-abbrev">Molecules</journal-id>
<journal-id journal-id-type="publisher-id">molecules</journal-id>
<journal-title-group><journal-title>Molecules</journal-title>
</journal-title-group>
<issn pub-type="epub">1420-3049</issn>
<publisher><publisher-name>MDPI</publisher-name>
</publisher>
</journal-meta>
<article-meta><article-id pub-id-type="pmid">31151235</article-id>
<article-id pub-id-type="pmc">6600397</article-id>
<article-id pub-id-type="doi">10.3390/molecules24112065</article-id>
<article-id pub-id-type="publisher-id">molecules-24-02065</article-id>
<article-categories><subj-group subj-group-type="heading"><subject>Article</subject>
</subj-group>
</article-categories>
<title-group><article-title>Design, Synthesis, Antimicrobial, and Anticancer Activities of Acridine Thiosemicarbazides Derivatives</article-title>
</title-group>
<contrib-group><contrib contrib-type="author"><name><surname>Chen</surname>
<given-names>Rui</given-names>
</name>
<xref ref-type="aff" rid="af1-molecules-24-02065">1</xref>
<xref ref-type="aff" rid="af2-molecules-24-02065">2</xref>
</contrib>
<contrib contrib-type="author"><name><surname>Huo</surname>
<given-names>Lini</given-names>
</name>
<xref ref-type="aff" rid="af1-molecules-24-02065">1</xref>
<xref rid="c1-molecules-24-02065" ref-type="corresp">*</xref>
</contrib>
<contrib contrib-type="author"><name><surname>Jaiswal</surname>
<given-names>Yogini</given-names>
</name>
<xref ref-type="aff" rid="af3-molecules-24-02065">3</xref>
</contrib>
<contrib contrib-type="author"><name><surname>Huang</surname>
<given-names>Jiayong</given-names>
</name>
<xref ref-type="aff" rid="af1-molecules-24-02065">1</xref>
</contrib>
<contrib contrib-type="author"><name><surname>Zhong</surname>
<given-names>Zhenguo</given-names>
</name>
<xref ref-type="aff" rid="af1-molecules-24-02065">1</xref>
</contrib>
<contrib contrib-type="author"><name><surname>Zhong</surname>
<given-names>Jing</given-names>
</name>
<xref ref-type="aff" rid="af1-molecules-24-02065">1</xref>
</contrib>
<contrib contrib-type="author"><contrib-id contrib-id-type="orcid" authenticated="true">https://orcid.org/0000-0003-0886-5204</contrib-id>
<name><surname>Williams</surname>
<given-names>Leonard</given-names>
</name>
<xref ref-type="aff" rid="af3-molecules-24-02065">3</xref>
</contrib>
<contrib contrib-type="author"><name><surname>Xia</surname>
<given-names>Xing</given-names>
</name>
<xref ref-type="aff" rid="af1-molecules-24-02065">1</xref>
</contrib>
<contrib contrib-type="author"><name><surname>Liang</surname>
<given-names>Yan</given-names>
</name>
<xref ref-type="aff" rid="af4-molecules-24-02065">4</xref>
</contrib>
<contrib contrib-type="author"><name><surname>Yan</surname>
<given-names>Zhenshuo</given-names>
</name>
<xref ref-type="aff" rid="af1-molecules-24-02065">1</xref>
</contrib>
</contrib-group>
<aff id="af1-molecules-24-02065"><label>1</label>
College of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530222, China;<email>58251323@163.com</email>
(R.C.);<email>hjyshjy@126.com</email>
(J.H.);<email>gxtcmuzzg@163.com</email>
(Z.Z.);<email>zhongjing1212@163.com</email>
(J.Z.);<email>xiaxing66@163.com</email>
(X.X.);<email>yanzhenshuo8@163.com</email>
(Z.Y.)</aff>
<aff id="af2-molecules-24-02065"><label>2</label>
Faculty of Chinese Medicine Science, Guangxi University of Chinese Medicine, Nanning 530222, China</aff>
<aff id="af3-molecules-24-02065"><label>3</label>
Center for Excellence in Post-Harvest Technologies, North Carolina A&T State University, The North Carolina Research Campus, 500 Laureate Way, Kannapolis, NC-28081, USA;<email>yoginijaiswal@gmail.com</email>
(Y.J.);<email>llw@ncat.edu</email>
(L.W.)</aff>
<aff id="af4-molecules-24-02065"><label>4</label>
College of Pharmacy, Guangxi Medical University, Nanning 530021, China;<email>vincyliang@163.com</email>
</aff>
<author-notes><corresp id="c1-molecules-24-02065"><label>*</label>
Correspondence: <email>huolini@126.com</email>
; Tel.: +86-07714953513</corresp>
</author-notes>
<pub-date pub-type="epub"><day>30</day>
<month>5</month>
<year>2019</year>
</pub-date>
<pub-date pub-type="collection"><month>6</month>
<year>2019</year>
</pub-date>
<volume>24</volume>
<issue>11</issue>
<elocation-id>2065</elocation-id>
<history><date date-type="received"><day>03</day>
<month>5</month>
<year>2019</year>
</date>
<date date-type="accepted"><day>24</day>
<month>5</month>
<year>2019</year>
</date>
</history>
<permissions><copyright-statement>© 2019 by the authors.</copyright-statement>
<copyright-year>2019</copyright-year>
<license license-type="open-access"><license-p>Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (<ext-link ext-link-type="uri" xlink:href="http://creativecommons.org/licenses/by/4.0/">http://creativecommons.org/licenses/by/4.0/</ext-link>
).</license-p>
</license>
</permissions>
<abstract><p><bold>Background:</bold>
Acridine and thiourea derivatives are important compounds in medicinal chemistry due to their diverse biological properties including anticancer and antimicrobial effects. However, literature reveals some side effects associated with use of acridines. It is suggested that hybrid molecules may reduce the side effects and enhance the beneficial properties due to synergistic activity. The objectives of the present study are to synthesize and evaluate the anticancer and antimicrobial properties of new hybrids of acridine thiosemicarbazides derivatives. <bold>Results:</bold>
The structures of the synthesized compounds <bold>4a–4e</bold>
were elucidated by MS and NMR spectra. In antimicrobial assay, Compound <bold>4c</bold>
exhibited potent antimicrobial activity compared to the other four compounds. In anticancer studies, we observed that compounds <bold>4a</bold>
, <bold>4b</bold>
, <bold>4d</bold>
and <bold>4e</bold>
exhibited high cytotoxicity against the MT-4 cell line, with IC50 values of 18.42 ± 1.18, 15.73 ± 0.90, 10.96 ± 0.62 and 11.63 ± 0.11 μM, respectively. The evaluation of anticancer effects, and the associated mechanism reveals that, the anticancer activities may be related to Topo I inhibitory activity, apoptosis and cell-cycle. Molecular docking studies revealed that the presence of planar naphtho-fused rings and a flexible thiourea group together, could improve DNA-intercalation and inhibition of DNA-Topo I activity. <bold>Conclusions:</bold>
The results of this study demonstrate that the rational design of target derivatives as novel antimicrobial or antitumor leads is feasible.</p>
</abstract>
<kwd-group><kwd>acridine</kwd>
<kwd>thiosemicarbazides</kwd>
<kwd>anticancer</kwd>
<kwd>antimicrobial</kwd>
</kwd-group>
</article-meta>
</front>
</pmc>
</record>
Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Sante/explor/ChloroquineV1/Data/Pmc/Curation
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 000714 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Pmc/Curation/biblio.hfd -nk 000714 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien |wiki= Sante |area= ChloroquineV1 |flux= Pmc |étape= Curation |type= RBID |clé= PMC:6600397 |texte= Design, Synthesis, Antimicrobial, and Anticancer Activities of Acridine Thiosemicarbazides Derivatives }}
Pour générer des pages wiki
HfdIndexSelect -h $EXPLOR_AREA/Data/Pmc/Curation/RBID.i -Sk "pubmed:31151235" \ | HfdSelect -Kh $EXPLOR_AREA/Data/Pmc/Curation/biblio.hfd \ | NlmPubMed2Wicri -a ChloroquineV1
![]() | This area was generated with Dilib version V0.6.33. | ![]() |