Synthesis, antitumor and anti-HIV-1 testing of certain thieno [2,3-d]pyrimidine, thieno[2,3-d]imidazo[1,2-c]pyrimidine and thieno[2,3-d][1,3] thiazine derivatives

被引:0
|
作者
Shehata, IA [1 ]
ElSubbagh, HI [1 ]
Abdelal, AM [1 ]
ElSherbeny, MA [1 ]
AlObaid, AA [1 ]
机构
[1] KING SAUD UNIV,COLL PHARM,DEPT PHARMACEUT CHEM,RIYADH 11451,SAUDI ARABIA
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中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of tetrahydrobenzo[b]thieno[2,3-d]pyrimidines, thieno[3,2-e]imidazo[1,2-c]pyrimidines and thieno[2,3-d][1,3]thiazines was synthesized as antitumor, antiviral agents. Compounds (2) under bar, (3) under bar and <(17)under bar> possessed moderate Anti-HIN-1 potency with EC(50) values ranging from 1.83 x 10(-5) to 3.42 x 10(-5) molar concentrations. All of the tested compounds showed cytotoxic effects (log GI(50) less than or equal to -4.0) against the growth of a variety of human tumor cell lines, including those derived from solid tumors. Compounds (3) under bar and (7) under bar showed strong potency while compounds <(11)under bar> and <(16)under bar> exhibited moderate activity. The detailed synthesis, spectroscopic and biological data are reported.
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页码:148 / 163
页数:16
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