A new class of pyrrolo[l,4lbenzodiazepine (PBD) analogues featuring a pyrazolo[4,3-e]pyrrolo- [l72-al[l,4]diazepinone ring system has been designed and synthesized. These compounds, 2a-0, 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.
Synthesis and Antitumor Activity of a New Class of Pyrazolo[4,3-e]pyrrolo[1,2-a][1,4]diazepinone Analogs of Pyrrolo[1,4][2,1-c]benzodiazepines
BARALDI, Pier Giovanni;CACCIARI, Barbara;MANFREDINI, Stefano;SIMONI, Daniele;
1994
Abstract
A new class of pyrrolo[l,4lbenzodiazepine (PBD) analogues featuring a pyrazolo[4,3-e]pyrrolo- [l72-al[l,4]diazepinone ring system has been designed and synthesized. These compounds, 2a-0, 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.File in questo prodotto:
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