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Mol Divers. 2013 Aug;17(3):435-44. doi: 10.1007/s11030-013-9442-1. Epub 2013 Apr 24.

Synthesis and in vitro cytotoxic evaluation of novel N-(3,4,5-trimethoxyphenyl)pyridin-2(1H)-one derivatives.

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1
Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai, 200062, China.

Abstract

A series of novel [Formula: see text]-(3,4,5-trimethoxyphenyl)pyridin-2([Formula: see text])-one derivatives were designed, synthesized, and evaluated for their in vitro cytotoxicity against human colon cancer cells HCT-116. The key steps involved consecutive Chan-Lam- and Buchwald-Hartwig couplings. Most of these C-6 substituted pyridone derivatives showed moderate antiproliferative activity. The preliminary SAR indicated that the conformationally restricted pyridones exhibited more potent cytotoxicity than the flexible counterparts. In addition, cell cycle analysis of the selected compounds 4b and e showed a G2/M arrest, suggesting a possible antitubulin mechanism for these novel pyridone derivatives.

PMID:
23612851
DOI:
10.1007/s11030-013-9442-1
[Indexed for MEDLINE]
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