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Open AccessArticle

Design, Synthesis and Biological Evaluation of 1,4-Disubstituted-3,4-dihydroisoquinoline Compounds as New Tubulin Polymerization Inhibitors

School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China
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Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Jurriaan Huskens
Int. J. Mol. Sci. 2015, 16(5), 10173-10184; https://doi.org/10.3390/ijms160510173
Received: 10 March 2015 / Revised: 28 April 2015 / Accepted: 29 April 2015 / Published: 5 May 2015
(This article belongs to the Section Materials Science)
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. View Full-Text
Keywords: 1,4-disubstituted-3,4-dihydroisoquinoline; tubulin polymerization inhibitor; antitumor agent 1,4-disubstituted-3,4-dihydroisoquinoline; tubulin polymerization inhibitor; antitumor agent
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Zhang, L.; Song, Y.; Huang, J.; Liu, J.; Zhu, W.; Zhou, Y.; Lv, J.; Zheng, C.; Zhu, J. Design, Synthesis and Biological Evaluation of 1,4-Disubstituted-3,4-dihydroisoquinoline Compounds as New Tubulin Polymerization Inhibitors. Int. J. Mol. Sci. 2015, 16, 10173-10184.

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