SEMISYNTHETIC SQUALESTATINS - SQUALENE SYNTHASE INHIBITION AND ANTIFUNGAL ACTIVITY - THE SAR OF C6 AND C7 MODIFICATIONS

被引：18

作者：

GIBLIN, GMP

BELL, R

HANCOCK, AP

HARTLEY, CD

INGLIS, GGA

PAYNE, JJ

PROCOPIOU, PA

SHINGLER, AH

SMITH, C

SPOONER, SJ

机构：

[1] Departments of Medicinal Chemistry, Glaxo Group Research, Greenford

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(01)80724-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We describe herein a protection/deprotectiOn strategy that enables efficient transformation of natural Squalestatin S1 into C6 and C7 acyl analogues. We present the mammalian and fungal SQS enzyme activity and whole cell antifungal activity of the semi-synthetic Squalestatins.

引用

页码：2605 / 2610

页数：6

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