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
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
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收藏
页码:1247 / 1252
页数:6
相关论文
共 15 条
[1]   STRUCTURE + SYNTHESIS OF DISTAMYCIN A [J].
ARCAMONE, F ;
NICOLELL.V ;
PENCO, S ;
OREZZI, P ;
PIRELLI, A .
NATURE, 1964, 203 (494) :1064-+
[2]   DESIGN, SYNTHESIS, DNA-BINDING, AND BIOLOGICAL-ACTIVITY OF A SERIES OF DNA MINOR-GROOVE-BINDING INTERCALATING DRUGS [J].
BAILLY, C ;
POMMERY, N ;
HOUSSIN, R ;
HENICHART, JP .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1989, 78 (11) :910-917
[3]  
BARALDI PG, UNPUB BIOORG MED CHE
[4]  
BROGGINI M, 1994, ANTI-CANCER DRUG DES, V9, P373
[5]  
BROGGINI M, 1991, CANCER RES, V51, P199
[6]  
DIMARCO A, 1962, CANCER CHEMOTH REP, P15
[7]   SYNTHESIS OF POTENTIAL ANTICANCER AGENTS .12. NITROGEN MUSTARDS FROM P-AMINOBENZOIC ACID DERIVATIVES [J].
ELDERFIELD, R ;
LIAO, TK .
JOURNAL OF ORGANIC CHEMISTRY, 1961, 26 (12) :4996-&
[8]  
FONTANA M, 1992, ANTI-CANCER DRUG DES, V7, P131
[9]   NMR CHARACTERIZATION OF A HETEROCOMPLEX FORMED BY DISTAMYCIN AND ITS ANALOG 2-IMD WITH D(CGCAAGTTGGC)-D(GCCAACTTGCG) - PREFERENCE FOR THE 1/1/1 2-IMD-DST-DNA COMPLEX OVER THE 2/1 2-IMD-DNA AND THE 2/1 DST-DNA COMPLEXES [J].
GEIERSTANGER, BH ;
DWYER, TJ ;
BATHINI, Y ;
LOWN, JW ;
WEMMER, DE .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1993, 115 (11) :4474-4482
[10]  
GERONI C, 1993, INT J CANCER, V68, P916