Synthesis and antitumor activity of new sulfonamide derivatives of thiadiazolo [3,2-a]pyrimidines

被引：148

作者：

El-Sayed, Nadia S. ^{[1
]}

El-Bendary, Eman R. ^{[1
]}

El-Ashry, Saadia M. ^{[1
]}

El-Kerdawy, Mohammed M. ^{[1
]}

机构：

[1] Univ Mansoura, Fac Pharm, Dept Med Chem, Mansoura 35516, Egypt

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 09期

关键词：

Sulfonamide derivatives; 1,3,4]Thiadiazolo[3,2-a]pyrimidines; DNA-binding affinity; Antitumor activity; CARBONIC-ANHYDRASE INHIBITORS; ISOZYME-IX; XII; AGENTS; TRANSMEMBRANE; EXPRESSION; ANALOGS;

D O I：

10.1016/j.ejmech.2011.05.037

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New series of sulfonamide derivatives of [1,3,4]thiadiazolo[3,2-a]pyrimidine were synthesized and investigated as antitumor agents. Some of the newly prepared compounds were tested for their in vitro and in vivo antitumor activities. Preliminary biological studies revealed that compounds 4c, 4f, and 4j exhibited the highest affinity to DNA, while compounds 4h,i, 6a-c, 8 and 12-14 exhibited moderate activity. Also, compounds 4j, 4f and 4c showed the highest percentage increase in lifespan of mice inoculated with Ehrlich ascites cells over 5-flurouracil (positive control). The detailed synthesis, spectroscopic and biological data are reported. (C) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：3714 / 3720

页数：7

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