1027392-37-5Relevant articles and documents
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents
Li, Wen-Tai,Hwang, Der-Ren,Chen, Ching-Ping,Shen, Chien-Wei,Huang, Chen-Long,Chen, Tung-Wei,Lin, Chi-Hung,Chang, Yee-Ling,Chang, Ying-Ying,Lo, Yue-Kan,Tseng, Huan-Yi,Lin, Chu-Chung,Song, Jeng-Shin,Chen, Hua-Chien,Chen, Shu-Jen,Wu, Se-Hui,Chen, Chiung-Tong
, p. 1706 - 1715 (2003)
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 IC50 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 (IC50 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.
