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

被引：34

作者：

Huang, Sheng-Xiong ^{[1
]}

Powell, Emily ^{[2
]}

Rajski, Scott R. ^{[1
]}

Zhao, Li-Xing ^{[4
]}

Jiang, Cheng-Lin ^{[4
]}

Duan, Yanwen ^{[6
]}

Xu, Wei

Shen, Ben ^{[1
,3
,5
]}

机构：

[1] Univ Wisconsin, Div Pharmaceut Sci, Madison, WI 53705 USA

[2] Univ Wisconsin, McArdle Lab Canc Res, Madison, WI 53705 USA

[3] Univ Wisconsin, Dept Chem, Madison, WI 53705 USA

[4] Yunnan Univ, Yunnan Inst Microbiol, Kunming 650091, Yunnan, Peoples R China

[5] Univ Wisconsin, Univ Wisconsin Natl Cooperat Drug Discovery Grp, Madison, WI 53705 USA

[6] Hunan Engn Res Ctr Combinatorial Biosynth & Nat P, Changsha 410329, Hunan, Peoples R China

来源：

ORGANIC LETTERS | 2010年 / 12卷 / 15期

关键词：

PAECILOMYCES SP FO-3684; KURASOIN-A; MULTIFUNCTIONAL MEDICINES; BETA; ANTIESTROGENS; MODULATORS; ALPHA;

D O I：

10.1021/ol1013526

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

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.

引用

页码：3525 / 3527

页数：3

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