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|Title:||Synthesis and cytotoxic activity of some novel N-pyridinyl-2-(6- phenylimidazo[2,1-b]thiazol-3-yl)acetamide derivatives|
|Citation:||Ding, H., Chen, Z., Zhang, C., Xin, T., Wang, Y., Song, H., Jiang, Y., Chen, Y., Xu, Y., Tan, C. (2012-04). Synthesis and cytotoxic activity of some novel N-pyridinyl-2-(6- phenylimidazo[2,1-b]thiazol-3-yl)acetamide derivatives. Molecules 17 (4) : 4703-4716. ScholarBank@NUS Repository. https://doi.org/10.3390/molecules17044703|
|Abstract:||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). © 2012 by the authors.|
|Appears in Collections:||Staff Publications|
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