SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL C-4 AZIRIDINE-BEARING PACLITAXEL (TAXOL) ANALOGS

被引：15

作者：

CHEN, SH

FAIRCHILD, C

LONG, BH

机构：

[1] Bristol-Myers Squibb Co., Princeton, NJ 08543

[2] Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 38卷 / 12期

关键词：

D O I：

10.1021/jm00012a029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Three novel C-4 aziridine-bearing paclitaxel analogs, 3-5, have been synthesized during the course of our continuing effort at C-4 modification. The key step in the synthesis is the aziridine ring formation at the C-4 position via an intramolecular Mitsunobu reaction. The syntheses and the biological evaluation of these C-4 aziridine-containing derivatives are herein discussed.

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页码：2263 / 2267

页数：5

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