New family of potential oncostatics: 2-Chloroethylnitrososulfamides (CENS) .1. Synthesis, structure, and pharmacological evaluation - (Preliminary results)

被引：47

作者：

Abdaoui, M

Dewynter, G

Aouf, N

Favre, G

Morere, A

Montero, JL

机构：

[1] UNIV MONTPELLIER 2,CNRS,LAB CHIM BIOMOL,F-34095 MONTPELLIER 5,FRANCE

[2] CLAUDIUS REGAUD INST MED ONCOL,F-31052 TOULOUSE,FRANCE

[3] UNIV ANNABA,DEPT CHEM,EL HADJAR,ALGERIA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1996年 / 4卷 / 08期

关键词：

nitrososulfamide; carboxylsulfamide; chlorosulfonyl isocyanate; Mitsunobu reaction; alkylating agent; oncostatics; chloroethylnitrosoureas; biological screening; A549; MCF7;

D O I：

10.1016/0968-0896(96)00118-6

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A new series of alkylating agents, 2-chloroethylnitrososulfamides (CENS), were developed on the model of 2-chloroethylnitrosoureas. Starting from chlorosulfonyl isocyanate, a four-step synthesis (carbamoylation-sulfamoylation, Mitsunobu alkylation, deprotection, and nitrosation) gives the title compounds in a 47-58% overall yield. The selection of the nitrosation site can be directed through an alternative route. The pharmacological evaluation shows a significant oncostatic activity towards both A549 and MCF7 cell lines. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：1227 / 1235

页数：9

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