对Bcl-2功能具有特异性抑制活性的四癌菌素衍生物的合成。
Synthesis of tetrocarcin derivatives with specific inhibitory activity towards Bcl-2 functions.
作者信息
Kaneko M, Nakashima T, Uosaki Y, Hara M, Ikeda S, Kanda Y
机构信息
Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd, Machida, Tokyo, Japan.
出版信息
Bioorg Med Chem Lett. 2001 Apr 9;11(7):887-90. doi: 10.1016/s0960-894x(01)00094-4.
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.
摘要
最近发现四癌菌素A是Bcl-2抗凋亡功能的抑制剂。我们合成了新型四癌菌素衍生物，以增强其对Bcl-2的选择性抑制活性。结果发现，21-乙酰氧基-9-糖氧基衍生物具有强大的Bcl-2抑制活性，且无明显抗菌活性。
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