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  • Title: Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
    Author: Li WT, Hwang DR, Chen CP, Shen CW, Huang CL, Chen TW, Lin CH, Chang YL, Chang YY, Lo YK, Tseng HY, Lin CC, Song JS, Chen HC, Chen SJ, Wu SH, Chen CT.
    Journal: J Med Chem; 2003 Apr 24; 46(9):1706-15. PubMed ID: 12699388.
    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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