A novel approach to the synthesis of cytotoxic C2-C3 unsaturated pyrrolo[2,1-c]benzodiazepines (PBDs) with conjugated acrylyl C2-substituents

Zhizhi Chen, Stephen J. Gregson, Philip W. Howard, David E. Thurston

Research output: Contribution to journalArticlepeer-review

20 Citations (Scopus)

Abstract

A concise synthesis of three novel C2–C3 unsaturated pyrrolo[2,1-c][1,4]benzodiazepine analogues (18–20) containing conjugated acrylyl C2-substituents is reported that utilises Heck coupling to install the C2-acrylyl side chains. These analogues possess significant cytotoxicity according to the NCI 60-cell line screen with 18 surpassing anthramycin (1) in potency.
Original languageEnglish
Pages (from-to)1547-1549
Number of pages3
JournalBioorganic & medicinal chemistry letters
Volume14
Issue number6
DOIs
Publication statusPublished - 22 Mar 2004

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