Synthesis and biological evaluation of novel series of thieno[2,3-d]pyrimidine derivatives as anticancer and antimicrobial agents

被引：19
|
作者：
Habib, Nargues S. [1 ]
Soliman, Raafat [1 ]
El-Tombary, Alaa A. [1 ]
El-Hawash, Soad A. [1 ]
Shaaban, Omaima G. [1 ]
机构：
[1] Univ Alexandria, Dept Pharmaceut Chem, Fac Pharm, Alexandria 21521, Egypt
来源：
MEDICINAL CHEMISTRY RESEARCH | 2013年 / 22卷 / 07期
关键词：
Thieno[2,3-d]pyrimidine; Synthesis; Anticancer; Antimicrobial; ANTITUMOR; ANALOGS; THIENOPYRIMIDINE; INHIBITORS; DISCOVERY;
D O I：
10.1007/s00044-012-0324-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The present study is concerned with the synthesis, anticancer and antimicrobial screening of several new 3-substituted or 2,3-disubstituted-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxamide derivatives. Three compounds (4b, 8c, and 11b) were selected by the National Cancer Institute and were first evaluated at a single-dose primary anticancer assay against 60 human cancer cell lines for their in vitro anticancer activity. Compound 8c which passed the criteria for activity in this assay was evaluated against the full panel of 60 human cancer cell lines at five concentrations at tenfold dilutions where it showed non-selective broad-spectrum activity against all cancer cell lines. Furthermore, compounds 4b, 6, 8c, 8d, and 16 showed pronounced antibacterial activities comparable to ampicillin against P. aeruginosa. Therefore, it was concluded that compound 8c may serve as a useful lead compound in search for powerful dual anticancer-antimicrobial agents.
引用
收藏
页码：3289 / 3308
页数：20
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