Design, Synthesis, and Biological Evaluation of Coumarin-Triazole Hybrid Molecules as Potential Antitumor and Pancreatic Lipase Agents

被引:45
作者
Kahveci, Bahittin [1 ]
Yilmaz, Fatih [2 ]
Mentese, Emre [2 ]
Ulker, Serdar [3 ]
机构
[1] Karadeniz Tech Univ, Dept Nutr & Diethet, Fac Hlth Sci, Trabzon, Turkey
[2] Recep Tayyip Erdogan Univ, Fac Arts & Sci, Dept Chem, TR-53100 Rize, Turkey
[3] Recep Tayyip Erdogan Univ, Fac Arts & Sci, Dept Biol, Rize, Turkey
关键词
Antitumor; Coumarin; Hybrid molecule; Lipase inhibition; Triazol-3-one; MICROWAVE-ASSISTED SYNTHESIS; TUMOR-CELL-LINES; 1,2,4-TRIAZOLE DERIVATIVES; ANTIFUNGAL ACTIVITY; ANTICANCER AGENTS; ANTIBACTERIAL ACTIVITY; ASSAY; INHIBITORS; APOPTOSIS; PLANTS;
D O I
10.1002/ardp.201600369
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The design, synthesis, and investigation of antitumor and anti-lipase activities of some coumarin-triazole hybrid molecules are reported. The synthesis of these hybrid molecules was performed under microwave irradiation and conventional heating procedures. The newly synthesized hybrid molecules were investigated as inhibitors against four tumor cell lines (BT20 human breast carcinoma, SK-Mel 128 melanoma, DU-145 prostate carcinoma, and A549 lung carcinoma) and porcine pancreatic lipase (PPL). Most of these compounds showed notable antitumor activities against the tested tumor cell lines, and compounds 8i and 8l showed the best anti-lipase activity of 99.30 +/- 0.56% and 99.85 +/- 1.21%, respectively, at a concentration of 10 mu M.
引用
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页数:9
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