European Journal of Medicinal Chemistry 2013-02-01

Diminutive effect on T and B-cell proliferation of non-cytotoxic α-santonin derived 1,2,3-triazoles: a report.

Praveen K Chinthakindi, Payare L Sangwan, Saleem Farooq, Rajeshwar R Aleti, Anupurna Kaul, Ajit K Saxena, Y L N Murthy, Ram A Vishwakarma, Surrinder Koul

文献索引：Eur. J. Med. Chem. 60 , 365-75, (2013)

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摘要

α-Santonin derived new series of 1,2,3-triazoles synthesized through Azide-Alkyne Huisgen 1,3-dipolar cycloaddition reaction between substituted aryl azide and a propargylated α-desmotrosantonin were bio-evaluated for their diminutive effect on ConA induced T-cell and LPS induced B-cell proliferation. Interestingly, most of the synthesized compounds showed better immunosuppressant activity than α-santonin. Triazole derivatives 9, 10, 17, 18, 29, and 30 displayed significant diminutive effect on cell proliferation. Compounds 12 and 13 were found selective against ConA T-cell proliferation exhibiting >90% inhibition at 1 × 10(-6) M concentration. The present study resulted in identification of several triazole derivatives as effective immunosuppressive agents.Copyright © 2012 Elsevier Masson SAS. All rights reserved.