Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes

Hsueh Yun Lee, Chih Yi Chang, Mei Jung Lai, Hsun Yueh Chuang, Ching Chuan Kuo, Chi Yen Chang, Jang Yang Chang, Jing Ping Liou

研究成果: Article同行評審

16 引文 斯高帕斯(Scopus)

摘要

This study reports the synthesis of a series of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes, which are potent antitubulin agents. Compound 13, (2-hydroxy-3,4,5-trimethoxyphenyl)-(6-methoxy-1H-indol-3-yl)-methanone exhibits marked antiproliferative activity against KB and MKN45 cells with IC50 values of 8.8 and 10.5 nM, respectively, binds strongly to the colchicine binding site and leads to inhibition of tubulin polymerization. It also behaves as a vascular disrupting agent which suppresses the formation of capillaries. The C2-OH group in the A-ring of this compound not only retains the biological activity but has valuable physicochemical properties.

原文English
頁(從 - 到)4230-4236
頁數7
期刊Bioorganic and Medicinal Chemistry
23
發行號15
DOIs
出版狀態Published - 2015 七月 23

All Science Journal Classification (ASJC) codes

  • 生物化學
  • 分子醫學
  • 分子生物學
  • 藥學科學
  • 藥物發現
  • 臨床生物化學
  • 有機化學

指紋

深入研究「Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes」主題。共同形成了獨特的指紋。

引用此