Synthesis, stereochemistry confirmation and biological activity evaluation of a constituent from Isodon excisus |
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Authors: | Xuechao XingPei Ho Geoffroy BourquinLi-An Yeh Gregory D Cuny |
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Institution: | Laboratory for Drug Discovery in Neurodegeneration, Brigham and Women's Hospital and Harvard Medical School, 65 Landsdowne St., Cambridge, MA 02139, USA |
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Abstract: | A synthesis and stereochemistry confirmation of a constituent recently isolated from the whole plant Isodon excisus is reported. An enantioselective catalytic boron-mediated reduction of an α-bromoketone was utilized in the key synthetic transformation. The methodology described herein was also used for the synthesis of the natural product's enantiomer and several derivatives. In addition, the compounds were evaluated for inhibitory activity in a caspase induction assay. The natural product was found to be devoid of activity, but several derivatives had moderate inhibitory activity (EC50<1 μM). |
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Keywords: | apoptosis caspase-induction inhibitor boron Isodon excisus |
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