THE CONTRIBUTION TO BINDING OF THE PYRANOSIDE SUBSTITUENTS IN THE EXCISED BINDING DOMAIN OF FK-506

被引：7

作者：

STOCKS, MJ

BIRKINSHAW, TN

TEAGUE, SJ

机构：

[1] Fisons Pharmaceuticals PLC, Loughborough, LE11 ORH, Bakewell Road

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(01)80513-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The contributions of the C-ll methyl and C-13 / C-15 methoxy substituents to the affinity of FK-506 for the immunophilin FKBP-12 were investigated. Subtraction of the C-11 methyl group led to a 400-fold drop in affinity. Removal of the C-13 and C-15 methoxy substituents led to a much smaller drop in affinity.

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页码：1457 / 1460

页数：4

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