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

15 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

    指紋

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

引用此

Lee, H. Y., Chang, C. Y., Lai, M. J., Chuang, H. Y., Kuo, C. C., Chang, C. Y., Chang, J. Y., & Liou, J. P. (2015). Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes. Bioorganic and Medicinal Chemistry, 23(15), 4230-4236. https://doi.org/10.1016/j.bmc.2015.06.043