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

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• 作者：Jingfang Qian-Cutrone ; Stella Huang ; Yue-Zhong Shu ; Dolatrai Vyas ; Craig Fairchild ; Ana Menendez ; Kimberly Krampitz ; Richard Dalterio ; Steven E Klohr ; and Qi Gao
• 刊名：Journal of the American Chemical Society
• 出版年：2002
• 出版时间：December 11, 2002
• 年：2002
• 卷：124
• 期：49
• 页码：14556 - 14557
• 全文大小：81K
• 年卷期：v.124,no.49(December 11, 2002)
• ISSN：1520-5126

文摘

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.