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.

Abstract:

: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.

journal_name

Bioorg Med Chem Lett

authors

Baraldi PG,Cacciari B,Romagnoli R,Spalluto G,Boyce CW,Boger DL

doi

10.1016/s0960-894x(99)00533-8

subject

Has Abstract

pub_date

1999-11-01 00:00:00

pages

3087-92

issue

21

eissn

0960-894X

issn

1464-3405

pii

S0960894X99005338

journal_volume

9

pub_type

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