Synthesis, anticancer and antibacterial evaluation of novel (isopropylidene) uridine-[1,2,3]triazole hybrids

被引:18
|
作者
Thatipamula, Ranjith Kumar [1 ]
Narsimha, Sirassu [1 ]
Battula, Kumaraswamy [1 ]
Chary, V. Rajendra [2 ]
Mamidala, Estari [2 ]
Reddy, Nagavelli Vasudeva [1 ]
机构
[1] Kakatiya Univ, Dept Chem, Warangal 506009, Telangana State, India
[2] Dept Zool, Infect Dis & Metab Disorders Res Lab, Warangal 506009, Telangana State, India
关键词
Uridine; 1,2,3-Triazole; Anticancer; Antibacterial activity; BIOLOGICAL EVALUATION; 1,2,3-TRIAZOLES; INHIBITORS; DERIVATIVES; POTENT; NUCLEOSIDES; ANALOGS; DESIGN; VIRUS; ACID;
D O I
10.1016/j.jscs.2015.12.001
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of novel (isopropylidene) uridine-[1,2,3]triazole hybrids (3a-3n) were efficiently synthesized via the copper-catalyzed azide-alkyne cycloaddition (CuAAC) from N-propargyl 2',3'-O-(isopropylidene) uridine with different aryl azides. All the synthesized compounds were screened for their in vitro anticancer and antibacterial activities. The anticancer activity results revealed that compounds 3d and 3f have registered equipotent activity against MCF-7 and 3n has shown excellent activity against HeLa in comparison with the standard drug Cisplatin. Remaining compounds have shown moderate to good anticancer activity against MCF-7 and HeLa cell lines. The antibacterial activity screening results revealed that, compounds 3b and 3n have shown excellent inhibition against Escherichia coli and Bacillus subtilis, 3d against Proteus vulgaris, 3k against Staphylococcus aureus and 3l against S. aureus and B. subtilis have shown equipotent activity in comparison with the standard drug Streptomycin. (C) 2015 King Saud University. Production and hosting by Elsevier B.V.
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页码:795 / 802
页数:8
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