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

Luke A. Masterson, Stephen J. Croker, Terence C. Jenkins, Philip W. Howard, David E. Thurston

Research output: Contribution to journalArticlepeer-review

26 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)901-904
Number of pages4
JournalBioorganic & medicinal chemistry letters
Volume14
Issue number4
DOIs
Publication statusPublished - 23 Feb 2004

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