A new class of pyrrolo[1,4]benzodiazepines (PBDs) analogs featuring a pyrazolo[4,3-e]pyrrolo[1,2-a][1,4]diazepinone ring system has been designed and synthesized. In these compds. the A-benzene ring, characteristic of PBDs, has been replaced by a dimethylpyrazole ring, a modification suggested by modeling studies performed on the PBD base structure. Biol. evaluation revealed appreciable antitumor activity for I and II (8.84-22.4 μM) which encourages further investigation of the N6 or N7 alkyl pyrazole analogs.
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]benzodiazepines (PBDs)
BARALDI, Pier Giovanni;CACCIARI, Barbara;MANFREDINI, Stefano;SIMONI, Daniele
1993
Abstract
A new class of pyrrolo[1,4]benzodiazepines (PBDs) analogs featuring a pyrazolo[4,3-e]pyrrolo[1,2-a][1,4]diazepinone ring system has been designed and synthesized. In these compds. the A-benzene ring, characteristic of PBDs, has been replaced by a dimethylpyrazole ring, a modification suggested by modeling studies performed on the PBD base structure. Biol. evaluation revealed appreciable antitumor activity for I and II (8.84-22.4 μM) which encourages further investigation of the N6 or N7 alkyl pyrazole analogs.File in questo prodotto:
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