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

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.

Graphical abstractSynthesis of a new series of triazole derivatives of α-santonin and their bioevaluation for T-cell and LPS-induced B-cell proliferation effect. Identification of potent immunosuppressive agents.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Synthesis of 30 α-santonin derivatives. ► Several derivatives were found immunosuppressive agents. ► The molecules showed diminutive effect on ConA T-cell and LPS-induced B-cell proliferation.