Synthesis and antitumor activity of substituted triazolo[4,3-a]pyrimidin-6-sulfonamide with an incorporated thiazolidinone moiety

被引：65
作者：
Hafez, Hend N. [1 ]
El-Gazzar, Abdel-Rahman B. A. [1 ]
机构：
[1] Natl Res Ctr, Photochem Dept, Heterocycl & Nucleoside Unit, Cairo 12622, Egypt
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 15期
关键词：
Triazolo[4,3-a]pyrimidine; Thioglycolic acid; Thiazolidinone; Anti-tumor; NATIONAL-CANCER-INSTITUTE; DRUG DISCOVERY; DERIVATIVES; ANTIOXIDANT; ANALOGS; DESIGN;
D O I：
10.1016/j.bmcl.2009.05.126
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Chlorosulfonation of 3-methyl[1,2,4]triazolo[4,3-a]pyrimidine with chlorosulfonic acid in the presence of thionyl chloride was studied. When triazolo[4,3-a]pyrimidines are used as substrates, the substitution occurs at C-6. Also the reactivity of the hydrazides (7) towards aldehydes, thioglycolic acid and amines were studies. The newly prepared compounds 10a,d and 11a,d demonstrated inhibitory effects on the growth of a wide range of cancer cell lines generally at 10 (5) M level and in some cases at 10 (7) M concentrations. (C) 2009 Elsevier Ltd. All rights reserved.
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收藏
页码：4143 / 4147
页数：5
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