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)

被引：14

作者：

BARALDI, PG ^{[1
]}

LEONI, A ^{[1
]}

CACCIARI, B ^{[1
]}

MANFREDINI, S ^{[1
]}

SIMONI, D ^{[1
]}

机构：

[1] UNIV BOLOGNA,DIPARTIMENTO SCI FARMACEUT,I-40126 BOLOGNA,ITALY

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 12期

关键词：

ANTHRAMYCIN; PYRAZOLO[4,3-E]PYRROLO[1,2-A][1,4]DIAZEPINONE ANALOGS; ANTITUMOR ACTIVITY; SYNTHESIS;

D O I：

10.1016/S0960-894X(01)80707-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 In these compounds the A-benzene ring, characteristic of PBDs, has been replaced by a dimethylpyrazole ring, a modification suggested by modelling studies performed on the PBD base structure.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

引用

页码：2511 / 2514

页数：4

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