2. Academic Validation
  3. 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

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

  • J Med Chem. 1994 Dec 9;37(25):4329-37. doi: 10.1021/jm00051a009.
P G Baraldi 1,  A Leoni,  B Cacciari,  S Manfredini,  D Simoni,  M Bergomi,  E Menta,  S Spinelli
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.
PMID: 7996544 DOI: 10.1021/jm00051a009
Abstract

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.

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