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Structure-guided optimization of estrogen receptor binding affinity and antagonist potency of pyrazolopyrimidines with basic side chains

Academic Article
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Overview

authors

  • Zhou, H. B.
  • Sheng, S. B.
  • Compton, D. R.
  • Kim, Y.
  • Joachimiak, A.
  • Sharma, S.
  • Carlson, K. E.
  • Katzenellenbogen, B. S.
  • Nettles, Kendall
  • Greene, G. L.
  • Katzenellenbogen, J. A.

publication date

  • January 2007

journal

  • Journal of Medicinal Chemistry  Journal

abstract

  • 2,3-Diarylpyrazolo[1,5-a]pyrimidines are estrogen receptor (ER) antagonists of modest potency that we have described previously. Guided by the crystal structure of an ER-ligand complex that we have obtained with one of these compounds, we prepared analogs that contain a basic side chain at the 2- or 3-aryl group and quickly found one that, according to the structure-based prediction, shows an increase in binding affinity and antagonist potency and a loss of residual agonist activity.

subject areas

  • Cell Line, Tumor
  • Crystallography, X-Ray
  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Humans
  • Ligands
  • Models, Molecular
  • Molecular Structure
  • Pyrazoles
  • Pyrimidines
  • Radioligand Assay
  • Structure-Activity Relationship
  • Transcriptional Activation
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Identity

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/jm061035y

PubMed ID

  • 17228884
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Additional Document Info

start page

  • 399

end page

  • 403

volume

  • 50

issue

  • 2

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