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Synthesis of tetrocarcin derivatives with specific inhibitory activity towards Bcl-2 functions
M Kaneko1, T Nakashima, Y Uosaki
1Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd, Machida, Tokyo, Japan. masami.kaneko@kyowa.co.jp
Bioorganic & Medicinal Chemistry Letters
|April 11, 2001
Abstract:
Tetrocarcin A was recently identified as an inhibitor of the anti-apoptotic function of Bcl-2. We synthesized novel tetrocarcin derivatives in order to increase their selective inhibitory activity against Bcl-2. It was found that 21-acetoxy-9-glycosyloxy derivatives had potent Bcl-2 inhibitory activity without significant antimicrobial activity.