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Discovery and total synthesis of a new estrogen receptor heterodimerizing actinopolymorphol a from actinopolymorpha rutilus

Academic Article
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Overview

authors

  • Huang, S. X.
  • Powell, E.
  • Rajski, S. R.
  • Zhao, L. X.
  • Jiang, C. L.
  • Duan, Y. W.
  • Xu, W.
  • Shen, Ben

publication date

  • August 2010

journal

  • Organic Letters  Journal

abstract

  • Estrogen receptor ERalpha and ERbeta 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 ERalpha/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.

subject areas

  • Acetates
  • Actinomycetales
  • Estrogen Receptor Modulators
  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Molecular Structure
  • Phenols
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Identity

PubMed Central ID

  • PMC2913291

International Standard Serial Number (ISSN)

  • 1523-7060

Digital Object Identifier (DOI)

  • 10.1021/ol1013526

PubMed ID

  • 20593804
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Additional Document Info

start page

  • 3525

end page

  • 3527

volume

  • 12

issue

  • 15

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