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Synthesis and biological evaluation of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) C8 cyclic amine conjugates.

Abstract：

:We report examples of a series of novel pyrrolo[2,1-c][1,4]benzodiazepine (PBD) analogues 12-15 prepared from a common functionalized building block 11 that can be conveniently synthesized on a large scale and in optically pure form. Isoindoline analogue 15 is the most cytotoxic agent in this series, has the highest DNA-binding affinity, and shows significant activity in the in vivo hollow fibre assay.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Masterson LA,Croker SJ,Jenkins TC,Howard PW,Thurston DE

doi

10.1016/j.bmcl.2003.12.017

subject

Has Abstract

pub_date

2004-02-23 00:00:00

pages

901-4

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960894X03013015

journal_volume

14

pub_type

杂志文章

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