Resolution of a CPzI precursor, synthesis and biological evaluation of (+) and (-)-N-Boc-CPzI: A further validation of the relationship between chemical solvolytic stability and cytotoxicity

被引：14

作者：

Baraldi, PG ^{[1
]}

Cacciari, B

Romagnoli, R

Spalluto, G

Boyce, CW

Boger, DL

机构：

[1] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy

[2] Univ Trieste, Dipartimento Sci Farmaceut, I-34127 Trieste, Italy

[3] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(99)00533-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The chemical resolution, using N-tosyl-L-proline as a chiral auxiliary, of a racemate of the pyrazole analog (=/-)-N-Boc-CPzI of the left hand segment (CPI) of the antitumor agent CC-1065, and the cytotoxic evaluation of both enantiomers are described. The reported results further validate the direct relationship between chemical solvolytic stability of the cyclopropane ring and cytotoxicity proposed by Boger and coworkers. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：3087 / 3092

页数：6

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