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

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

Publication date

March 2004

DOI

10.1016/j.bmcl.2003.12.094

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

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

Abstract

Extracted data

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

Abstract

Extracted data

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