Design,Synthesis and Biological Evaluation of 1,4-Disubstituted-3,4-dihydroisoquinoline Compounds as New Tubulin Polymerization Inhibitors |
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| Authors: | Ling Zhang Yunlong Song Jingjing Huang Jia Liu Wenwen Zhu Youjun Zhou Jiaguo Lv Canhui Zheng Ju Zhu |
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| Affiliation: | School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China; E-Mails: (L.Z.); (Y.S.); (J.H.); (J.L.); (W.Z.); (Y.Z.); (J.L.) |
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| Abstract: | A series of 1,4-disubstituted-3,4-dihydroisoquinoline derivatives designed as tubulin polymerization inhibitors were synthesized. Their cytotoxic activities against the CEM leukemia cell line were evaluated. Most of them displayed moderate cytotoxic activities, and compounds 21 and 32 showed good activities with IC50 of 4.10 and 0.64 μM, respectively. The most potent compound 32 was further confirmed to be able to inhibit tubulin polymerization, and its hypothetical binding mode with tubulin was obtained by molecular docking. |
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| Keywords: | 1 4-disubstituted-3 4-dihydroisoquinoline tubulin polymerization inhibitor antitumor agent |
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