Synthesis and in vitro cytotoxic evaluation of novel -(3,4,5-trimethoxyphenyl)pyridin-2()-one derivatives
文献类型：期刊论文
| 作者 | Chen, Taijie1; Luo, Yu1; Sheng, Li3; Li, Jia3 ; Hu, Youhong3; Lu, Wei2
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| 刊名 | MOLECULAR DIVERSITY
 |
| 出版日期 | 2013-08 |
| 卷号 | 17期号:3页码:435-444 |
| 关键词 | Pyridin-2(1H)-one Combretastatin A-4 Chan-Lam coupling reaction Buchwald-Hartwig coupling reaction HCT-116 Cytotoxicity Cell cycle |
| ISSN号 | 1381-1991 |
| DOI | 10.1007/s11030-013-9442-1 |
| 文献子类 | Article |
| 英文摘要 | 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. |
| WOS关键词 | COMBRETASTATIN A-4 DERIVATIVES ; 2-PYRIDONE DERIVATIVES ; ANTIMITOTIC AGENTS ; INHIBITORS ; DISCOVERY ; RECEPTOR ; POTENT ; PYRIDIN-2(1H)-ONE ; ANALOGS ; MOIETY |
| 资助项目 | National Natural Science Foundation of China[81172936] ; National Natural Science Foundation of China[21102046] ; Fundamental Research Funds for the Central Universities[00000000] ; Laboratory of Organic Functional Molecules, the Sino-French Institute of ECNU[00000000] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000321912600003 |
| 出版者 | SPRINGER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277523]  |
| 专题 | 国家新药筛选中心 药物化学研究室 药物安全性评价中心 |
| 通讯作者 | Luo, Yu |
| 作者单位 | 1.E China Normal Univ, Dept Chem, Shanghai 200062, Peoples R China; 2.E China Normal Univ, Inst Drug Discovery & Dev, Shanghai 200062, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, Taijie,Luo, Yu,Sheng, Li,et al. Synthesis and in vitro cytotoxic evaluation of novel -(3,4,5-trimethoxyphenyl)pyridin-2()-one derivatives[J]. MOLECULAR DIVERSITY,2013,17(3):435-444. |
| APA | Chen, Taijie,Luo, Yu,Sheng, Li,Li, Jia,Hu, Youhong,&Lu, Wei.(2013).Synthesis and in vitro cytotoxic evaluation of novel -(3,4,5-trimethoxyphenyl)pyridin-2()-one derivatives.MOLECULAR DIVERSITY,17(3),435-444. |
| MLA | Chen, Taijie,et al."Synthesis and in vitro cytotoxic evaluation of novel -(3,4,5-trimethoxyphenyl)pyridin-2()-one derivatives".MOLECULAR DIVERSITY 17.3(2013):435-444. |
入库方式： OAI收割
来源：上海药物研究所
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