Synthesis of the first examples of A-C8/C-C2 amide-linked pyrrolo [2, 1-c][1, 4] benzodiazepine dimers

SJ Gregson, PW Howard, DE Thurston

Index: Gregson, Stephen J.; Howard, Philip W.; Thurston, David E. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 14 p. 2277 - 2280

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Citation Number: 28

Abstract

We report the synthesis of novel A-C8/C-C2 amide-linked pyrrolo [2, 1-c][1, 4] benzodiazepine dimers (4a and 4b) via convergent routes. These compounds lack the potent DNA interstrand cross-linking ability and resultant pronounced cytotoxicity of the known A-C8/A-C8′ linked dimers (eg, 2a–b).