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Int. J. Mol. Sci. 2015, 16(5), 10173-10184; doi:10.3390/ijms160510173

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
These authors contributed equally to this work.
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Authors to whom correspondence should be addressed.
Academic Editor: Jurriaan Huskens
Received: 10 March 2015 / Revised: 28 April 2015 / Accepted: 29 April 2015 / Published: 5 May 2015
(This article belongs to the Section Biomaterial Sciences)
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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. 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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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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