THE VERSATILE STEROID NUCLEUS - DESIGN AND SYNTHESIS OF A PEPTIDOMIMETIC EMPLOYING THIS NOVEL SCAFFOLD

被引:46
作者
HIRSCHMANN, R
SPRENGELER, PA
KAWASAKI, T
LEAHY, JW
SHAKESPEARE, WC
SMITH, AB
机构
[1] Department of Chemistry, University of Pennsylvania, Philadelphia
关键词
D O I
10.1016/S0040-4020(01)90222-4
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The design and synthesis of peptidomimetic 1 employing the novel cyclopentanoperhydrophenanthrene skeleton is described. The large body of steroid literature allows for the introduction of diverse peptidal side chains with precise regio- and stereoselective control. Compound 1 binds to the fibrinogen receptor on blood platelets (GP IIb/IIIa), for which it was designed, with an IC50 of ca. 100 muM.
引用
收藏
页码:3665 / 3676
页数:12
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