In continuation of our endeavours to synthesize immunosuppressive agents from α-santonin, we report herein the design and synthesis of a new series of α-santonin derived O-aryl/aliphatic ether, ester and amide analogs and the evaluation of their immunosuppressive activities. The studies led to several analogs with significant immunosuppressive effects by inhibiting ConA and LPS stimulated T- and B-cell proliferation in a dose dependent manner. The more significant compounds , , , , and displayed potent inhibitory activity on the mitogen-induced T- and B-cell proliferation in comparison to α-santonin . Compound displayed stupendous immunosuppressive effects with ∼80% suppression of B and ∼75% suppression of T lymphocyte proliferation, respectively The investigation on BALB/c mice revealed that non-cytotoxic compound suppresses both humoral and cellular immunity.
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| http://dx.doi.org/10.1039/c6md00527f | DOI Listing |
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