Two classes of 1,4-disubstituted 1,2,3-triazoles were synthesized using one-pot reaction of α-tosyloxy ketones/α-halo ketones, sodium azide, and terminal alkynes in the presence of aq. PEG (1:1, v/v) using the click chemistry approach and evaluated for Src kinase inhibitory activity. Structure-activity relationship analysis demonstrated that insertion of C6H5- and 4-CH3C6H4- at position 4 for both classes and less bulkier aromatic group at position 1 in class 1 contribute critically to the modest Src inhibition activity (IC50 = 32-43 µM) of 1,4-disubstituted 1,2,3-triazoles.
Kumar, Dalip, et al. "Click chemistry inspired one-pot synthesis of 1, 4-disubstituted 1, 2, 3-triazoles and their Src kinase inhibitory activity." Bioorganic & medicinal chemistry letters 21.1 (2011): 449-452. doi: 10.1016/j.bmcl.2010.10.121
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