Discovery and Total Synthesis of a New Estrogen Receptor Heterodimerizing Actinopolymorphol A from Actinopolymorpha rutilus

作者:Huang Sheng Xiong; Powell Emily; Rajski Scott R; Zhao Li Xing; Jiang Cheng Lin; Duan Yanwen; Xu Wei; Shen Ben*
来源:Organic Letters, 2010, 12(15): 3525-3527.
DOI:10.1021/ol1013526

摘要

Estrogen receptor ER alpha and ER beta heterodimerization has been implicated in cancer chemoprevention. The discovery, structural elucidation, and total synthesis of a new natural product, actinopolymorphol A (1), from Actinopolymorpha rutilus (YIM45725) that preferentially induces ER alpha/beta heterodimerization is reported. Total synthesis of 1 has allowed us to determine Its absolute stereochemistry and that of a previously known deacetylated congener, and 1 represents the first member of a new class of natural products not previously recognized to modulate ER function.