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

页码：1247 / 1252

页数：6

共 15 条

[11] LEE HH, 1991, ANTI-CANCER DRUG DES, V6, P501
[12] EFFICIENT TOTAL SYNTHESES OF THE OLIGOPEPTIDE ANTIBIOTICS NETROPSIN AND DISTAMYCIN
LOWN, JW
KROWICKI, K
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1985, 50 (20) : 3774 - 3779
[13] BIOLOGICAL PROFILE OF FCE-24517, A NOVEL BENZOYL MUSTARD ANALOG OF DISTAMYCIN-A
PEZZONI, G
GRANDI, M
BIASOLI, G
CAPOLONGO, L
BALLINARI, D
GIULIANI, FC
BARBIERI, B
PASTORI, A
PESENTI, E
MONGELLI, N
SPREAFICO, F
[J]. BRITISH JOURNAL OF CANCER, 1991, 64 (06) : 1047 - 1050
[14] Pinner A., 1877, CHEM BER-RECL, V10, P1889
[15] CARBOXY DERIVATIVES OF SULFONAMIDOTHIAZOLES
SPRAGUE, JM
LINCOLN, RM
ZIEGLER, C
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1946, 68 (02) : 266 - 269

← 1 2 →