Date of Original Version
Biomedical and Pharmaceutical Sciences
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.
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Kumar, D., Reddy, V. B., Kumar, A., Mandal, D., Tiwari, R., & Parang, K. (2011). 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), 449-452. doi: 10.1016/j.bmcl.2010.10.121
Available at: https://doi.org/10.1016/j.bmcl.2010.10.121
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