Synthesis and biological activity of A-nor-paclitaxel analogues

被引：17

作者：

Chordia, MD

Kingston, DGI

Hamel, E

Lin, CM

Long, BH

Fairchild, CA

Johnston, KA

Rose, WC

机构：

[1] NCI,FREDERICK CANC RES & DEV CTR,LAB DRUG DISCOVERY RES & DEV,DEV THERAPEUT PROGRAM,FREDERICK,MD 21702

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1997年 / 5卷 / 05期

关键词：

D O I：

10.1016/S0968-0896(97)00035-7

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A number of paclitaxel analogues with a 5-membered A-ring (A-nor-paclitaxels, or (15 right-arrow 1)-abeo-paclitaxels) have been prepared in order to determine whether analogues of this class might have improved bioactivity as compared with paclitaxel. Most of the compounds synthesized were less active than paclitaxel, but one analogue was equivalent to paclitaxel in a tubulin-assembly assay, and another analogue was more cytotoxic than paclitaxel in two different cell lines of the NCI screen.

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页码：941 / 947

页数：7

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