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


KAHVECİ B., Yilmaz F., Mentese E., ULKER S.

ARCHIV DER PHARMAZIE, vol.350, no.8, 2017 (Peer-Reviewed Journal) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 350 Issue: 8
  • Publication Date: 2017
  • Doi Number: 10.1002/ardp.201600369
  • Journal Name: ARCHIV DER PHARMAZIE
  • Journal Indexes: Science Citation Index Expanded, Scopus
  • Keywords: 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

Abstract

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.