TAXOL(R) STRUCTURE-ACTIVITY-RELATIONSHIPS - SYNTHESIS AND BIOLOGICAL EVALUATION OF TAXOL ANALOGS MODIFIED AT C-7

被引：27

作者：

CHEN, SH ^{[1
]}

KANT, J ^{[1
]}

MAMBER, SW ^{[1
]}

ROTH, GP ^{[1
]}

WEI, JM ^{[1
]}

MARSHALL, D ^{[1
]}

VYAS, DM ^{[1
]}

FARINA, V ^{[1
]}

CASAZZA, A ^{[1
]}

LONG, BH ^{[1
]}

ROSE, WC ^{[1
]}

JOHNSTON, K ^{[1
]}

FAIRCHILD, C ^{[1
]}

机构：

[1] BRISTOL MYERS SQUIBB CO,PHARMACEUT RES INST,PRINCETON,NJ 08543

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(00)80075-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of taxol derivatives, modified at C-7, is described. This includes sulfonate, silylether, ester, carbonate, carbamate, fluoro, dehydro and deoxy derivatives. Biological evaluation shows that these modifications do not usually significantly compromise activity. However, none of the C-7 analogs prepared thus far have been shown to be better than taxol in both in vitro and in vivo assays.

引用

页码：2223 / 2228

页数：6

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