Synthesis and antitumor activity of a new class of pyrazolo[4,3- e]pyrrolo[1,2-a][1,4]diazepinone analogues of pyrrolo[1,4][2,1- c]benzodiazepines

Article abstract of DOI:10.1021/jm00051a009

A new class of pyrrolo[1,4]benzodiazepine (PBD) analogues featuring a pyrazolo[4,3-e]pyrrolo[1,2-a][1,4]diazepinone ring system has been designed and synthesized. These compounds, 2a-o, are characterized by the substitution of the aromatic A ring, characteristic of the PBDs, with a disubstituted pyrazole ring bearing alkyl and benzyl substituents at N₆ or N₇ and alkyl or carbomethoxy substituents at C₈. Biological evaluation revealed an appreciable in vitro cytotoxic activity for compounds 2a,b,f-i.