2-Amino-3,4,5-Trimethoxybenzophenones as Potent Tubulin Polymerization Inhibitors

Hsun Yueh Chuang, Jang-Yang Chang, Mei Jung Lai, Ching Chuan Kuo, Hsueh Yun Lee, Hsing Pang Hsieh, Ying Jen Chen, Li Tzong Chen, Wen Yu Pan, Jing Ping Liou

研究成果: Article

12 引文 斯高帕斯(Scopus)

摘要

A series of novel 2-amino-3,4,5-trimethoxybenzophenone analogues exhibited excellent activity as tubulin polymerization inhibitors by targeting the colchicine binding site of microtubules. The lead compound 17 exhibited an IC50 value of 1.6μM, similar to that of combretastatin A-4 (IC50=1.9μM). It also displayed remarkable anti-proliferative activity, with IC50 values ranging from 7-16nM against a variety of human cancer cell lines and one MDR(+) cancer cell line. SAR information indicated that the introduction of an amino group at the C2 position of benzophenone ringA and the C3' position of benzophenone ringB play important roles in maximizing activity.

原文English
頁(從 - 到)450-456
頁數7
期刊ChemMedChem
6
發行號3
DOIs
出版狀態Published - 2011 三月 7

    指紋

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

引用此

Chuang, H. Y., Chang, J-Y., Lai, M. J., Kuo, C. C., Lee, H. Y., Hsieh, H. P., Chen, Y. J., Chen, L. T., Pan, W. Y., & Liou, J. P. (2011). 2-Amino-3,4,5-Trimethoxybenzophenones as Potent Tubulin Polymerization Inhibitors. ChemMedChem, 6(3), 450-456. https://doi.org/10.1002/cmdc.201000479