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Molecules 2012, 17(4), 4703-4716;

Synthesis and Cytotoxic Activity of Some Novel N-Pyridinyl-2-(6-phenylimidazo[2,1-b]thiazol-3-yl)acetamide Derivatives

School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
The Key Laboratory of Chemical Biology, Guangdong Province, Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055, China
Bioinformatics and Drug Design Group, Department of Computational Science, National University of Singapore, Blk SOC1, Level 7, 3 Science Drive 2, Singapore 117543, Singapore
Authors to whom correspondence should be addressed.
Received: 29 February 2012 / Revised: 1 April 2012 / Accepted: 13 April 2012 / Published: 23 April 2012
(This article belongs to the Section Medicinal Chemistry)
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A series of novel compounds bearing imidazo[2,1-b]thiazole scaffolds were designed and synthesized based on the optimization of the virtual screening hit compound N-(6-morpholinopyridin-3-yl)-2-(6-phenylimidazo[2,1-b]thiazol-3-yl)acetamide (5a), and tested for their cytotoxicity against human cancer cell lines, including HepG2 and MDA-MB-231. The results indicated that the compound 2-(6-(4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl)-N-(6-(4-(4-methoxybenzyl)piperazin-1-yl)pyridin-3-yl)acetamide (5l), with slightly higher inhibition on VEGFR2 than 5a (5.72% and 3.76% inhibitory rate at 20 μM, respectively), was a potential inhibitor against MDA-MB-231 (IC50 = 1.4 μM) compared with sorafenib (IC50 = 5.2 μM), and showed more selectivity against MDA-MB-231 than HepG2 cell line (IC50 = 22.6 μM). View Full-Text
Keywords: imidazo[2,1-b]thiazoles; cytotoxic activity; synthesis imidazo[2,1-b]thiazoles; cytotoxic activity; synthesis

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Ding, H.; Chen, Z.; Zhang, C.; Xin, T.; Wang, Y.; Song, H.; Jiang, Y.; Chen, Y.; Xu, Y.; Tan, C. Synthesis and Cytotoxic Activity of Some Novel N-Pyridinyl-2-(6-phenylimidazo[2,1-b]thiazol-3-yl)acetamide Derivatives. Molecules 2012, 17, 4703-4716.

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