1,2,3-Triazole-nimesulide hybrid: Their design,synthesis and evaluation as potential anticancer agents |
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| Authors: | Jyoti Mareddy N Suresh C Ganesh Kumar Ravikumar Kapavarapu A Jayasree Sarbani Pal |
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| Institution: | 1. Department of Chemistry, MNR Degree & PG College, Kukatpally, Hyderabad 500085, India;2. Centre for Chemical Sciences and Technology, Institute of Science & Technology, Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad 500085, India;3. Chemical Biology Laboratory, Medicinal Chemistry and Pharmacology Division, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India;4. Doctoral Programme in Experimental Biology and Biomedicine, Center for Neuroscience and Cell Biology, Institute for Interdisciplinary Research, University of Coimbra (IIIUC), 3004-517 Coimbra, Portugal |
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| Abstract: | A new hybrid template has been designed by integrating the structural features of nimesulide and the 1,2,3-triazole moiety in a single molecular entity at the same time eliminating the problematic nitro group of nimesulide. The template has been used for the generation of a library of molecules as potential anticancer agents. A mild and greener CuAAC approach has been used to synthesize these compounds via the reaction of 4-azido derivative of nimesulide and terminal alkynes in water. Three of these compounds showed promising growth inhibition (IC50 ～6–10 μM) of A549, HepG2, HeLa and DU145 cancer cell lines but no significant effects on HEK293 cell line. They also inhibited PDE4B in vitro (60–70% at 10 μM) that was supported by the docking studies (PLP score 87–94) in silico. |
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| Keywords: | Nimesulide 1 2 3-Triazole Azide Alkyne Anticancer activity |
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