Synthesis and cytotoxic evaluation for some new 2,5-disubstituted pyrimidine derivatives for anticancer activity

被引:17
|
作者
Reddy, Onteddu Surendranatha [1 ]
Suryanarayana, Ch. Venkata [2 ]
Narayana, K. J. P. [3 ]
Anuradha, V. [2 ]
Babu, B. Hari [1 ]
机构
[1] Acharya Nagarjuna Univ, Dept Chem, Guntur, Andhra Pradesh, India
[2] Vignan Sch PG Studies, Dept Chem, Guntur, Andhra Pradesh, India
[3] Acharya Nagarjuna Univ, Dept Microbiol, Guntur, Andhra Pradesh, India
关键词
2-Chloro-5-bromopyrimidine; Cesium carbonate; Green synthesis; HeLa cell line; PdCl2(PPh3)(2); CROSS-COUPLING REACTIONS; PALLADIUM CATALYSIS; SUZUKI REACTION; WATER; INHIBITORS; ACETATE; ACIDS;
D O I
10.1007/s00044-014-1276-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
An efficient synthetic approach for 2,5-disubstituted pyrimidines has been reported. The desired 2,5-substituted pyrimidines were obtained by Suzuki coupling of 2-substituted benzyloxy-5-bromopyrimidines with various aryl boronic acids in the presence catalytic amount of PdCl2(PPh3)(2) with 0.5 M aqueous Na2CO3 in water at 80 A degrees C. 2-Benzyloxy-5-bromopyrimidines were synthesized, in turn by the reaction of 2-chloro-5-bromopyrimidine with substituted benzyl alcohols in the presence of Cs2CO3 in CH3CN:DMF (1:1). Some of the 2,5-disubstituted pyrimidines have shown moderate in vitro cytotoxic activity against HeLa cell line.
引用
收藏
页码:1777 / 1788
页数:12
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