Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents

J Med Chem. 2003 Apr 24;46(9):1706-15. doi: 10.1021/jm020471r.

Wen-Tai Li ¹, Der-Ren Hwang, Ching-Ping Chen, Chien-Wei Shen, Chen-Long Huang, Tung-Wei Chen, Chi-Hung Lin, Yee-Ling Chang, Ying-Ying Chang, Yue-Kan Lo, Huan-Yi Tseng, Chu-Chung Lin, Jeng-Shin Song, Hua-Chien Chen, Shu-Jen Chen, Se-Hui Wu, Chiung-Tong Chen

Affiliations

Affiliation

1 Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 9F, 161, Sec. 6, Min-Chiuan East Road, Nei-Hu, Taipei 114, Taiwan, ROC.

PMID: 12699388 DOI: 10.1021/jm020471r

Abstract

A series of N-heterocyclic indolyl glyoxylamides were synthesized and evaluated for in vitro and in vivo Anticancer activities. They exhibited a broad spectrum of Anticancer activity not only in murine leukemic Cancer cells but also in human gastric, breast, and uterus Cancer cells as well as their multidrug resistant sublines with a wide range of IC(50) values. They also induced Apoptosis and caused DNA fragmentation in human gastric Cancer cells. Among the compounds studied, 7 showed the most potent activity of growth inhibition (IC(50) = 17-1711 nM) in several human Cancer cells. Given orally, compounds 7 and 13 dose-dependently prolonged the survival of Animals inoculated with P388 leukemic Cancer cells. N-Heterocyclic indolyl glyoxylamides may be useful as orally active chemotherapeutic agents against Cancer and refractory cancerous diseases of multidrug resistance phenotype.

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