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ID: ALA1137953

Journal: Bioorg Med Chem Lett

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

Authors: Chen Z, Gregson SJ, Howard PW, Thurston DE.

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.

CiteXplore: 15006400

DOI: 10.1016/j.bmcl.2003.12.094