Discovery, Synthesis and Antiproliferative Evaluation of Isosideroxylin, a Novel Isoflavone Derived from Leiophyllum buxifolium (Sand Myrtle)

摘要

Natural products from plants have been an important source in drug discovery throughout human history, especially in anticancer drug development. The New Jersey Pine Barrens (NJ pinelands) is a vast wild ecosystem from which little chemical or bioactivity exploration of the plants has been done. In our continuing search for naturally-occurring compounds with interesting biological activities, bioassay-guided fractionation of Leiophyllum buxifolium (sand myrtle) collected from the NJ pinelands, led to the isolation of a new C-methylisoflavone, isosideroxylin. This new compound displayed a selective antiproliferative effect against MDA-MB-231 cells, while showing weak inhibition against the MCF-7 cell line and no inhibition against the normal fibroblast cell line. To prepare for the SAR study and search for more potent analogs, a proof of concept study of the total synthetic route of isosideroxylin starting from phloroglucinol was developed.