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)期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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)

Authors:	Pier Giovanni Baraldi Alberto Leoni Barbara Cacciari Stefano Manfredini Daniele Simoni

Affiliation:	^a Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, I-44100 Ferrara, Italy ^b Dipartimento di Scienze Farmaceutiche, Università di Bologno, Via Belmeloro 6, I-40126 Bologna, Italia

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 In these compounds the A-benzene ring, characteristic of PBDs, has been replaced by a dimethylpyrazole ring, a modification suggested by modelling studies performed on the PBD base structure. Biological evaluation releaved appreciable antitumor activity for compounds 14 and 15 (8.84–22.4 μM) which encourages further investigation of the N⁶ and N⁷ alkyl pyrazole analogs.

Keywords:	anthramycin pyrazolo[4 3-e]pyrrolo[1 2-a][1 4]diazepinone analogs antitumor activity synthesis.
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