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Synthesis and Bilogical Activity of Novel Quinoline and Coumarin Hybrids Bridged by 1,2,3-triazole Ring

The field of drug discovery is constantly advancing in its quest to find new biologically active compounds. Recently, an emerging trend in medical chemistry is molecular hybridization, which is often used as a key strategy in drug design [1]. It includes combining known biologically active moieties as scaffolds to build a new molecule that could retain properties, or potentially have new activity. Coumarin and quinoline are widely used in pharmaceuticals, as well as in new molecular hybrids. Triazole ring are also important linkage, building block and pharmachophore in molecular hybrids with quinolines and coumarins [2, 3]. In this work, we present synthesis of novel hybrids of quinoline and coumarin bridged with 1, 2, 3-triazole ring. The methylazido coumarins were prepared by cyclization of corresponding phenols and ethyl 4-chloroacetoacetate, followed by azidation. The hybrids bridged with 1, 2, 3-triazole (1-35) were prepared using Cu-catalyzed Huisgen-1, 3-dipolar cycloaddition reaction. Antitumor activity of novel molecular hybrids was examined against human tumor cell lines: glioblastoma, pancreatic adenocarcinoma, colorectal carcinoma, lung carcinoma, acute lymphoblastic leukemia, acute myeloid leukemia, chronic myeloid leukemia and non-Hodgkin lymphoma. [1] G. Bérubé, Expert Opin. Drug Discov. 11 (2016) 281–305. [2] R. Reddyrajula. U. Dalimba, Chem. Select 4 (2019) 2685–2693. [3] K. Bhagat et. al., ACS Omega 4 (2019) 8720–8730

Quinoline hybrids, coumarin hybrids, 1, 2, 3-triazole, click chemistry, antitumor evaluation

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