Compounds having a,�-unsaturated lactones display a variety of biological activities. Many research groups have tested both natural and unnatural a,�-unsaturated lactones for as-yet undiscovered biological properties. We synthesized a,�-unsaturated lactones with various substituents at the d-position and studied their immunosuppressive effects, that is, the inhibition of Interleukin-2 (IL-2) production. Among the compounds synthesized, the benzofuran-substituted a,�-unsaturated lactone 4h showed the best inhibitory activity toward IL-2 production in Jurkat e6-1 T lymphocytes (IC50 = 66.9 nM) without cytotoxicity at 10 �M. The results indicated that 4h may be useful as a potent immunosuppressive agent, as well as in IL-2-related studies.

Synthesis and biological evaluation of α,β-unsaturated lactones as potent immunosuppressive agents

243rd National Meeting (2012)

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