Synthesis of novel, DNA binding heterocyclic dehydroabietylamine derivatives as potential antiproliferative and apoptosis-inducing agents
Identifieur interne : 000E70 ( Ncbi/Merge ); précédent : 000E69; suivant : 000E71Synthesis of novel, DNA binding heterocyclic dehydroabietylamine derivatives as potential antiproliferative and apoptosis-inducing agents
Auteurs : Fengyi Zhao [République populaire de Chine] ; Xu Sun [République populaire de Chine] ; Wen Lu [République populaire de Chine] ; Li Xu [République populaire de Chine] ; Jiuzhou Shi [République populaire de Chine] ; Shilong Yang [République populaire de Chine] ; Mengyi Zhou [République populaire de Chine] ; Fan Su [République populaire de Chine] ; Feng Lin [République populaire de Chine] ; Fuliang Cao [République populaire de Chine]Source :
- Drug Delivery [ 1071-7544 ] ; 2020.
Abstract
Several dehydroabietylamine derivatives containing heterocyclic moieties such as
thiophene and pyrazine ring were successfully synthesized. The antiproliferative
activities of these thiophene-based Schiff-bases, thiophene amides, and pyrazine amides
were investigated
Url:
DOI: 10.1080/10717544.2020.1716879
PubMed: 31984809
PubMed Central: 7034089
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as potential antiproliferative and apoptosis-inducing agents</title><author><name sortKey="Zhao, Fengyi" sort="Zhao, Fengyi" uniqKey="Zhao F" first="Fengyi" last="Zhao">Fengyi Zhao</name><affiliation wicri:level="1"><nlm:aff id="AF0001"><institution>Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation><affiliation wicri:level="1"><nlm:aff id="AF0002"><institution>College of Forestry, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation><affiliation wicri:level="1"><nlm:aff id="AF0003"><institution>College of Science, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Sun, Xu" sort="Sun, Xu" uniqKey="Sun X" first="Xu" last="Sun">Xu Sun</name><affiliation wicri:level="1"><nlm:aff id="AF0003"><institution>College of Science, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation><affiliation wicri:level="1"><nlm:aff id="AF0004"><institution>College of Information Science and Technology, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Lu, Wen" sort="Lu, Wen" uniqKey="Lu W" first="Wen" last="Lu">Wen Lu</name><affiliation wicri:level="1"><nlm:aff id="AF0003"><institution>College of Science, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Xu, Li" sort="Xu, Li" uniqKey="Xu L" first="Li" last="Xu">Li Xu</name><affiliation wicri:level="1"><nlm:aff id="AF0001"><institution>Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation><affiliation wicri:level="1"><nlm:aff id="AF0003"><institution>College of Science, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Shi, Jiuzhou" sort="Shi, Jiuzhou" uniqKey="Shi J" first="Jiuzhou" last="Shi">Jiuzhou Shi</name><affiliation wicri:level="1"><nlm:aff id="AF0003"><institution>College of Science, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Yang, Shilong" sort="Yang, Shilong" uniqKey="Yang S" first="Shilong" last="Yang">Shilong Yang</name><affiliation wicri:level="1"><nlm:aff id="AF0005"><institution>Advanced Analysis and Testing Center, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Zhou, Mengyi" sort="Zhou, Mengyi" uniqKey="Zhou M" first="Mengyi" last="Zhou">Mengyi Zhou</name><affiliation wicri:level="1"><nlm:aff id="AF0005"><institution>Advanced Analysis and Testing Center, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Su, Fan" sort="Su, Fan" uniqKey="Su F" first="Fan" last="Su">Fan Su</name><affiliation wicri:level="1"><nlm:aff id="AF0005"><institution>Advanced Analysis and Testing Center, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Lin, Feng" sort="Lin, Feng" uniqKey="Lin F" first="Feng" last="Lin">Feng Lin</name><affiliation wicri:level="1"><nlm:aff id="AF0005"><institution>Advanced Analysis and Testing Center, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Cao, Fuliang" sort="Cao, Fuliang" uniqKey="Cao F" first="Fuliang" last="Cao">Fuliang Cao</name><affiliation wicri:level="1"><nlm:aff id="AF0001"><institution>Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation><affiliation wicri:level="1"><nlm:aff id="AF0002"><institution>College of Forestry, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">PMC</idno><idno type="pmid">31984809</idno><idno type="pmc">7034089</idno><idno type="url">http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7034089</idno><idno type="RBID">PMC:7034089</idno><idno type="doi">10.1080/10717544.2020.1716879</idno><date when="2020">2020</date><idno type="wicri:Area/Pmc/Corpus">000495</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Corpus" wicri:corpus="PMC">000495</idno><idno type="wicri:Area/Pmc/Curation">000495</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Curation">000495</idno><idno type="wicri:Area/Pmc/Checkpoint">000038</idno><idno type="wicri:explorRef" wicri:stream="Pmc" wicri:step="Checkpoint">000038</idno><idno type="wicri:Area/Ncbi/Merge">000E70</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en" level="a" type="main">Synthesis of novel, DNA binding heterocyclic dehydroabietylamine derivatives
as potential antiproliferative and apoptosis-inducing agents</title><author><name sortKey="Zhao, Fengyi" sort="Zhao, Fengyi" uniqKey="Zhao F" first="Fengyi" last="Zhao">Fengyi Zhao</name><affiliation wicri:level="1"><nlm:aff id="AF0001"><institution>Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation><affiliation wicri:level="1"><nlm:aff id="AF0002"><institution>College of Forestry, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation><affiliation wicri:level="1"><nlm:aff id="AF0003"><institution>College of Science, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Sun, Xu" sort="Sun, Xu" uniqKey="Sun X" first="Xu" last="Sun">Xu Sun</name><affiliation wicri:level="1"><nlm:aff id="AF0003"><institution>College of Science, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation><affiliation wicri:level="1"><nlm:aff id="AF0004"><institution>College of Information Science and Technology, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Lu, Wen" sort="Lu, Wen" uniqKey="Lu W" first="Wen" last="Lu">Wen Lu</name><affiliation wicri:level="1"><nlm:aff id="AF0003"><institution>College of Science, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Xu, Li" sort="Xu, Li" uniqKey="Xu L" first="Li" last="Xu">Li Xu</name><affiliation wicri:level="1"><nlm:aff id="AF0001"><institution>Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation><affiliation wicri:level="1"><nlm:aff id="AF0003"><institution>College of Science, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Shi, Jiuzhou" sort="Shi, Jiuzhou" uniqKey="Shi J" first="Jiuzhou" last="Shi">Jiuzhou Shi</name><affiliation wicri:level="1"><nlm:aff id="AF0003"><institution>College of Science, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Yang, Shilong" sort="Yang, Shilong" uniqKey="Yang S" first="Shilong" last="Yang">Shilong Yang</name><affiliation wicri:level="1"><nlm:aff id="AF0005"><institution>Advanced Analysis and Testing Center, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Zhou, Mengyi" sort="Zhou, Mengyi" uniqKey="Zhou M" first="Mengyi" last="Zhou">Mengyi Zhou</name><affiliation wicri:level="1"><nlm:aff id="AF0005"><institution>Advanced Analysis and Testing Center, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Su, Fan" sort="Su, Fan" uniqKey="Su F" first="Fan" last="Su">Fan Su</name><affiliation wicri:level="1"><nlm:aff id="AF0005"><institution>Advanced Analysis and Testing Center, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Lin, Feng" sort="Lin, Feng" uniqKey="Lin F" first="Feng" last="Lin">Feng Lin</name><affiliation wicri:level="1"><nlm:aff id="AF0005"><institution>Advanced Analysis and Testing Center, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author><author><name sortKey="Cao, Fuliang" sort="Cao, Fuliang" uniqKey="Cao F" first="Fuliang" last="Cao">Fuliang Cao</name><affiliation wicri:level="1"><nlm:aff id="AF0001"><institution>Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation><affiliation wicri:level="1"><nlm:aff id="AF0002"><institution>College of Forestry, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea># see nlm:aff country strict</wicri:regionArea></affiliation></author></analytic><series><title level="j">Drug Delivery</title><idno type="ISSN">1071-7544</idno><idno type="eISSN">1521-0464</idno><imprint><date when="2020">2020</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en"><title>Abstract</title><p>Several dehydroabietylamine derivatives containing heterocyclic moieties such as
thiophene and pyrazine ring were successfully synthesized. The antiproliferative
activities of these thiophene-based Schiff-bases, thiophene amides, and pyrazine amides
were investigated <italic>in vitro</italic> against Hela (cervix), MCF-7 (breast), A549
(lung), HepG2 (liver), and HUVEC (umbilical vein) cells by MTT assay. The toxicity of
<bold>L<sup>1</sup></bold>−<bold>L<sup>10</sup></bold>(IC<sub>50</sub> = 5.92− >100 μM) was lower than <bold>L<sup>0</sup></bold>(1.27 μM) and DOX (4.40 μM) in every case. Compound <bold>L<sup>1</sup></bold> had higher
anti-HepG2 <bold>(</bold>0.66 μM), anti-MCF-7 (5.33 μM), and anti-A549 (2.11 μM) and
compound <bold>L<sup>3</sup></bold> had higher anti-HepG2 (1.63 μM) and anti-MCF-7
(2.65 μM) activities. Both of these compounds were recognized with high efficiency in
apoptosis induction in HepG2 cells and intercalated binding modes with DNA. Moreover, with
average IC<sub>50</sub> values of 0.66 and 5.98 μM, <bold>L<sup>1</sup></bold> was nine
times more effective at suppressing cultured HepG2 cells viability than normal cells (SI =
9). The relative tumor proliferation rate (T/C) was 38.6%, the tumor inhibition rate was
up to 61.2%, which indicated that <bold>L<sup>1</sup></bold> had no significant toxicity
but high anti-HepG2 activity <italic>in vivo</italic>. Thus, it may be a potential
antiproliferation drug with nontoxic side effects.</p></div></front><back><div1 type="bibliography"><listBibl><biblStruct><analytic><author><name sortKey="Ahmed, Hea" uniqKey="Ahmed H">HEA Ahmed</name></author><author><name sortKey="Ihmaid, Sk" uniqKey="Ihmaid S">SK Ihmaid</name></author><author><name sortKey="Omar, Am" uniqKey="Omar A">AM Omar</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Aissi, Re" uniqKey="Aissi R">RE Aissi</name></author><author><name sortKey="Liu, J" uniqKey="Liu J">J Liu</name></author><author><name sortKey="Besse, S" uniqKey="Besse S">S Besse</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Arjmand, F" uniqKey="Arjmand F">F Arjmand</name></author><author><name sortKey="Aziz, M" uniqKey="Aziz M">M Aziz</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Auxiliadora, Mda" uniqKey="Auxiliadora M">MDA Auxiliadora</name></author><author><name sortKey="Pablo, Br" 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<front><journal-meta><journal-id journal-id-type="nlm-ta">Drug Deliv</journal-id><journal-id journal-id-type="iso-abbrev">Drug Deliv</journal-id><journal-id journal-id-type="publisher-id">IDRD</journal-id><journal-id journal-id-type="publisher-id">idrd20</journal-id><journal-title-group><journal-title>Drug Delivery</journal-title></journal-title-group><issn pub-type="ppub">1071-7544</issn><issn pub-type="epub">1521-0464</issn><publisher><publisher-name>Taylor & Francis</publisher-name></publisher></journal-meta><article-meta><article-id pub-id-type="pmid">31984809</article-id><article-id pub-id-type="pmc">7034089</article-id><article-id pub-id-type="doi">10.1080/10717544.2020.1716879</article-id><article-id pub-id-type="publisher-id">1716879</article-id><article-categories><subj-group subj-group-type="heading"><subject>Research Article</subject></subj-group></article-categories><title-group><article-title>Synthesis of novel, DNA binding heterocyclic dehydroabietylamine derivatives
as potential antiproliferative and apoptosis-inducing agents</article-title><alt-title alt-title-type="running-authors">F. Zhao et al.</alt-title></title-group><contrib-group><contrib contrib-type="author"><name><surname>Zhao</surname><given-names>Fengyi</given-names></name><xref ref-type="aff" rid="AF0001"><sup>a</sup></xref><xref ref-type="aff" rid="AF0002"><sup>b</sup></xref><xref ref-type="aff" rid="AF0003"><sup>c</sup></xref></contrib><contrib contrib-type="author"><name><surname>Sun</surname><given-names>Xu</given-names></name><xref ref-type="aff" rid="AF0003"><sup>c</sup></xref><xref ref-type="aff" rid="AF0004"><sup>d</sup></xref></contrib><contrib contrib-type="author"><name><surname>Lu</surname><given-names>Wen</given-names></name><xref ref-type="aff" rid="AF0003"><sup>c</sup></xref></contrib><contrib contrib-type="author"><name><surname>Xu</surname><given-names>Li</given-names></name><xref ref-type="aff" rid="AF0001"><sup>a</sup></xref><xref ref-type="aff" rid="AF0003"><sup>c</sup></xref><xref ref-type="corresp" rid="AN0001"></xref></contrib><contrib contrib-type="author"><name><surname>Shi</surname><given-names>Jiuzhou</given-names></name><xref ref-type="aff" rid="AF0003"><sup>c</sup></xref></contrib><contrib contrib-type="author"><name><surname>Yang</surname><given-names>Shilong</given-names></name><xref ref-type="aff" rid="AF0005"><sup>e</sup></xref></contrib><contrib contrib-type="author"><name><surname>Zhou</surname><given-names>Mengyi</given-names></name><xref ref-type="aff" rid="AF0005"><sup>e</sup></xref></contrib><contrib contrib-type="author"><name><surname>Su</surname><given-names>Fan</given-names></name><xref ref-type="aff" rid="AF0005"><sup>e</sup></xref></contrib><contrib contrib-type="author"><name><surname>Lin</surname><given-names>Feng</given-names></name><xref ref-type="aff" rid="AF0005"><sup>e</sup></xref></contrib><contrib contrib-type="author"><name><surname>Cao</surname><given-names>Fuliang</given-names></name><xref ref-type="aff" rid="AF0001"><sup>a</sup></xref><xref ref-type="aff" rid="AF0002"><sup>b</sup></xref></contrib><aff id="AF0001"><label>a</label><institution>Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</aff><aff id="AF0002"><label>b</label><institution>College of Forestry, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</aff><aff id="AF0003"><label>c</label><institution>College of Science, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</aff><aff id="AF0004"><label>d</label><institution>College of Information Science and Technology, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country>;</aff><aff id="AF0005"><label>e</label><institution>Advanced Analysis and Testing Center, Nanjing Forestry University</institution>, Nanjing,<country>PR China</country></aff></contrib-group><author-notes><fn id="AUFN1"><p>Supplemental data for this article can be accessed <ext-link ext-link-type="uri" xlink:href="https://doi.org/10.1080/10717544.2020.1716879"><underline>here</underline></ext-link>.</p></fn><corresp id="AN0001">CONTACT Li Xu <email>2016qlsz@njfu.edu.cn</email><institution>Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing
Forestry University</institution>, Nanjing, 210037, <country>PR
China</country></corresp></author-notes><pub-date pub-type="collection"><year>2020</year></pub-date><pub-date pub-type="epub"><day>27</day><month>1</month><year>2020</year></pub-date><volume>27</volume><issue>1</issue><fpage seq="19">216</fpage><lpage>227</lpage><history><date date-type="received"><day>27</day><month>11</month><year>2019</year></date><date date-type="rev-recd"><day>05</day><month>1</month><year>2020</year></date><date date-type="accepted"><day>13</day><month>1</month><year>2020</year></date></history><permissions><copyright-statement>© 2020 The Author(s). Published by Informa UK Limited, trading as
Taylor & Francis Group.</copyright-statement><copyright-year>2020</copyright-year><copyright-holder>The Author(s)</copyright-holder><license license-type="open-access" xlink:href="http://creativecommons.org/licenses/by/4.0/"><license-p>This is an Open Access article distributed under the terms of the Creative
Commons Attribution 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>), which permits unrestricted
use, distribution, and reproduction in any medium, provided the original work is
properly cited.</license-p></license></permissions><self-uri content-type="pdf" xlink:href="IDRD_27_1716879.pdf"></self-uri><abstract><title>Abstract</title><p>Several dehydroabietylamine derivatives containing heterocyclic moieties such as
thiophene and pyrazine ring were successfully synthesized. The antiproliferative
activities of these thiophene-based Schiff-bases, thiophene amides, and pyrazine amides
were investigated <italic>in vitro</italic> against Hela (cervix), MCF-7 (breast), A549
(lung), HepG2 (liver), and HUVEC (umbilical vein) cells by MTT assay. The toxicity of
<bold>L<sup>1</sup></bold>−<bold>L<sup>10</sup></bold>(IC<sub>50</sub> = 5.92− >100 μM) was lower than <bold>L<sup>0</sup></bold>(1.27 μM) and DOX (4.40 μM) in every case. Compound <bold>L<sup>1</sup></bold> had higher
anti-HepG2 <bold>(</bold>0.66 μM), anti-MCF-7 (5.33 μM), and anti-A549 (2.11 μM) and
compound <bold>L<sup>3</sup></bold> had higher anti-HepG2 (1.63 μM) and anti-MCF-7
(2.65 μM) activities. Both of these compounds were recognized with high efficiency in
apoptosis induction in HepG2 cells and intercalated binding modes with DNA. Moreover, with
average IC<sub>50</sub> values of 0.66 and 5.98 μM, <bold>L<sup>1</sup></bold> was nine
times more effective at suppressing cultured HepG2 cells viability than normal cells (SI =
9). The relative tumor proliferation rate (T/C) was 38.6%, the tumor inhibition rate was
up to 61.2%, which indicated that <bold>L<sup>1</sup></bold> had no significant toxicity
but high anti-HepG2 activity <italic>in vivo</italic>. Thus, it may be a potential
antiproliferation drug with nontoxic side effects.</p></abstract><kwd-group kwd-group-type="author"><title>Keywords</title><kwd>Dehydroabietylamine derivatives</kwd><kwd>antiproliferative</kwd><kwd>lower toxicity</kwd><kwd>apoptosis</kwd></kwd-group><funding-group><award-group><funding-source><named-content content-type="funder-name">National Key Research and Development Program
of China</named-content><named-content content-type="funderidentifier">10.13039/501100002852</named-content></funding-source><award-id>706</award-id></award-group><award-group><funding-source><named-content content-type="funder-name">Sate Key Laboratory for Chemistry and
Molecular Engineering of Medicinal Resources (Guangxi Normal
University)</named-content></funding-source><award-id>-B06</award-id></award-group><funding-statement>This work was supported by the National Key Research and Development
Program of China [grant number 2017YFD0600706] and Sate Key Laboratory for Chemistry and
Molecular Engineering of Medicinal Resources (Guangxi Normal University) [grant number
CMEMR2017-B06].</funding-statement></funding-group><counts><fig-count count="7"></fig-count><table-count count="4"></table-count><page-count count="12"></page-count><word-count count="8137"></word-count></counts></article-meta></front></pmc><affiliations><list><country><li>République populaire de Chine</li></country></list><tree><country name="République populaire de Chine"><noRegion><name sortKey="Zhao, Fengyi" sort="Zhao, Fengyi" uniqKey="Zhao F" first="Fengyi" last="Zhao">Fengyi Zhao</name></noRegion><name sortKey="Cao, Fuliang" sort="Cao, Fuliang" uniqKey="Cao F" first="Fuliang" last="Cao">Fuliang Cao</name><name sortKey="Cao, Fuliang" sort="Cao, Fuliang" uniqKey="Cao F" first="Fuliang" last="Cao">Fuliang Cao</name><name sortKey="Lin, Feng" sort="Lin, Feng" uniqKey="Lin F" first="Feng" last="Lin">Feng Lin</name><name sortKey="Lu, Wen" sort="Lu, Wen" uniqKey="Lu W" first="Wen" last="Lu">Wen Lu</name><name sortKey="Shi, Jiuzhou" sort="Shi, Jiuzhou" uniqKey="Shi J" first="Jiuzhou" last="Shi">Jiuzhou Shi</name><name sortKey="Su, Fan" sort="Su, Fan" uniqKey="Su F" first="Fan" last="Su">Fan Su</name><name sortKey="Sun, Xu" sort="Sun, Xu" uniqKey="Sun X" first="Xu" last="Sun">Xu Sun</name><name sortKey="Sun, Xu" sort="Sun, Xu" uniqKey="Sun X" first="Xu" last="Sun">Xu Sun</name><name sortKey="Xu, Li" sort="Xu, Li" uniqKey="Xu L" first="Li" last="Xu">Li Xu</name><name sortKey="Xu, Li" sort="Xu, Li" uniqKey="Xu L" first="Li" last="Xu">Li Xu</name><name sortKey="Yang, Shilong" sort="Yang, Shilong" uniqKey="Yang S" first="Shilong" last="Yang">Shilong Yang</name><name sortKey="Zhao, Fengyi" sort="Zhao, Fengyi" uniqKey="Zhao F" first="Fengyi" last="Zhao">Fengyi Zhao</name><name sortKey="Zhao, Fengyi" sort="Zhao, Fengyi" uniqKey="Zhao F" first="Fengyi" last="Zhao">Fengyi Zhao</name><name sortKey="Zhou, Mengyi" sort="Zhou, Mengyi" uniqKey="Zhou M" first="Mengyi" last="Zhou">Mengyi Zhou</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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