Synthesis of novel, DNA binding heterocyclic dehydroabietylamine derivatives as potential antiproliferative and apoptosis-inducing agents
Identifieur interne : 000043 ( Main/Exploration ); précédent : 000042; suivant : 000044Synthesis 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
Affiliations:
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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 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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></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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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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