期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 1, 页码 449-452出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.10.121
关键词
Click chemistry; Triazoles; Src kinase; Protein tyrosine kinase; Structure-activity relationship
资金
- University Grants Commission (SAP, DRS)
- Birla Institute of Technology & Science, Pilani
- India National Science Foundation [CHE 0748555]
- American Cancer Society [RSG-07-290-01-CDD]
Two classes of 1,4-disubstituted 1,2,3-triazoles were synthesized using one-pot reaction of alpha-tosyloxy ketones/alpha-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 mu M) of 1,4-disubstituted 1,2,3-triazoles. (c) 2010 Elsevier Ltd. All rights reserved.
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