Stephacidin A and B:  Two Structurally Novel, Selective Inhibitors of the Testosterone-Dependent Prostate LNCaP Cells

Jingfang Qian‐Cutrone(Bristol-Myers Squibb (United States)), Stella Huang(Bristol-Myers Squibb (United States)), Yue‐Zhong Shu(Bristol-Myers Squibb (United States)), Dolatrai M. Vyas(Bristol-Myers Squibb (United States)), Craig R. Fairchild(Bristol-Myers Squibb (United States)), Ana T. Menendez(Bristol-Myers Squibb (United States)), Kimberly Krampitz(Bristol-Myers Squibb (United States)), R. A. Dalterio(Bristol-Myers Squibb (United States)), Steven E. Klohr(Bristol-Myers Squibb (United States)), Qi Gao(Bristol-Myers Squibb (United States))
Journal of the American Chemical Society
November 16, 2002
Cited by 222

Abstract

Two novel antitumor alkaloids, Stephacidin A and B, were isolated from the solid fermentation of Aspergillus ochraceus WC76466. Both alkaloids exhibit in vitro cytotoxicity against a number of human tumor cell lines; however, stephacidin B demonstrated more potent and selective antitumor activities, especially against prostate testeosterone-dependent LNCaP cells with IC50 value of 60 nM. The structures of stephacidin A and B were established on the basis of the NMR data and X-ray crystallography. With 15 rings and 9 chiral centers, stephacidin B represents one of the most structurally complex and novel alkaloids occurring in nature.


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