Document Type
Article
Publication Date
2011
Abstract
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.
Recommended Citation
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
Copyright
Elsevier
Creative Commons License
This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 4.0 License.
Included in
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Comments
NOTICE: this is the author’s version of a work that was accepted for publication in Bioorganic & Medicinal Chemistry Letters. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Bioorganic & Medicinal Chemistry Letters, volume 21, issue 1, in 2011. DOI: 10.1016/j.bmcl.2010.10.121
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