期刊
MOLECULAR DIVERSITY
卷 17, 期 3, 页码 435-444出版社
SPRINGER
DOI: 10.1007/s11030-013-9442-1
关键词
Pyridin-2(1H)-one; Combretastatin A-4; Chan-Lam coupling reaction; Buchwald-Hartwig coupling reaction; HCT-116; Cytotoxicity; Cell cycle
类别
资金
- National Natural Science Foundation of China [81172936, 21102046]
- Fundamental Research Funds for the Central Universities
- Laboratory of Organic Functional Molecules, the Sino-French Institute of ECNU
A series of novel -(3,4,5-trimethoxyphenyl)pyridin-2()-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.
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