Synthesis and biological evaluation of 4-(1,2,3-triazol-1-yl)coumarin derivatives as potential antitumor agents |
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| Affiliation: | 1. P.G. Department of Chemistry, P.C. Jabin Science College, Hubli 580031, Karnataka, India;2. P.G. Department of Studies and Research in Polymer Science, Sir, M.V. PG Centre, Mandya 571402, University of Mysore, Karnataka, India;3. Department of Physics, L.V.D. College, Raichur 584103, Karnataka, India;4. Department of Chemistry, L.V.D. College, Raichur 584103, Karnataka, India;1. Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad 431001, MS, India;2. Department of Biotechnology, Savitribai Phule Pune University, Pune 411007, MS, India;1. Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab 143005, India;2. Lloyd Institute of Management and Technology, Greater Noida, UP, India;3. Indian Institute of Integrative Medicine, Jammu, India;1. Department of Medicinal Chemistry, The University of Kansas, 1251 Wescoe Hall Drive, Malott Hall 4070, Lawrence, KS 66045-7563, USA;2. Department of Urology, The University of Kansas Medical Center, 3901 Rainbow Blvd., Mail Stop 1016, Kansas City, KS 66160, USA;1. School of Pharmacy, Anhui Medical University, Hefei 230032, PR China;2. Key Laboratory of Green Pesticide and Agriculture Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China;3. State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China;1. Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Italy;2. Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via S. Donato, 19/2, 40127 Bologna, Italy;3. National Institute of Biostructures and Biosystems, Via delle Medaglie D''oro, 305, 00136 Roma, Italy |
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| Abstract: | In this research, a series of 4-(1,2,3-triazol-1-yl)coumarin conjugates were synthesized and their anticancer activities were evaluated in vitro against three human cancer cell lines, including human breast carcinoma MCF-7 cell, colon carcinoma SW480 cell and lung carcinoma A549 cell. To increase the biological potency, structural optimization campaign was conducted focusing on the C-4 position of 1,2,3-triazole and the C-6, C-7 positions of coumarin. In addition, to further evaluate the role of 1,2,3-triazole and coumarin for antiproliferative activity, 9 compounds possessing 4-(piperazin-1-yl)coumarin framework and 3 derivatives baring quinoline core were also synthesized. By MTT assay in vitro, most of the compounds display attractive antitumor activities, especially 23. Further flow cytometry assays demonstrate that compound 23 exerts the antiproliferative role through arresting G2/M cell-cycle and inducing apoptosis. |
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| Keywords: | Coumarin Antiproliferative activity Apoptosis |
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