Structure-activity relationship of novel tallimustine derivatives: Synthesis and antitumor activity

被引：23
|
作者：
Baraldi, PG [1 ]
Beria, I [1 ]
Cacciari, B [1 ]
Capolongo, L [1 ]
Cozzi, P [1 ]
Mongelli, N [1 ]
Romagnoli, R [1 ]
Spalluto, G [1 ]
机构：
[1] PHARMACIA & UPJOHN, ONCOL PRECLIN RES, MILAN, ITALY
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 11期
关键词：
D O I：
10.1016/0960-894X(96)00205-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Oligopeptide-like derivatives structurally related to the antitumor agent tallimustine, where one or two pyrrole rings were replaced by pyrazole or thiazole rings and bearing benzoyl nitrogen mustard or bromoacryloyl moieties were synthesized and evaluated in vitro and in vivo against L1210 murine leukemia. Compounds 9 and 12 showed antitumor activity higher than or comparable with that of tallimustine. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码：1247 / 1252
页数：6
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