| Literature DB >> 12699388 |
Wen-Tai Li1, 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.
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.Entities:
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Year: 2003 PMID： 12699388 DOI： 10.1021/jm020471r
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446