Synthesis of derivatives of the novel cyclophilin-binding immunosuppressant sanglifehrin A with reduced numbers of polar functions

被引：9

作者：

Bänteli, R ^{[1
]}

Wagner, J ^{[1
]}

Zenke, G ^{[1
]}

机构：

[1] Novartis Pharma AG, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(01)00293-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The syntheses and the biological activities of 53-deoxo sanglifehrin A (2) and 61-deoxy octahydrosanglifehrin A (3) are described. Compound 2 shows intracellular cyclophilin (CyP)-binding and immunosuppressive activity in the mixed-lymphocyte reaction (MLR) similar to that of sanglifehrin A (1). Compound 3 is much less active in the MLR despite unchanged intracellular CyP-binding. This indicates that the 53-keto group is not necessary for immunosuppressive activity, while the 61 hydroxy group is required. (C) 2001 Published by Elsevier Science Ltd.

引用

页码：1609 / 1612

页数：4

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