Search results for: ESTROGEN%20RECEPTOR-BENZO%5BB%5DNAPHTHO%5B1

• Towards β-selectivity in functional estrogen receptor antagonists

  Publication

  • J. J. Rodríguez
  • K. Filipiak
  • M. Maslyk
  • J. Ciepielski
  • S. Demkowicz
  • S. de Pascual-Teresa
  • S. Martín-Santamaría
  • B. d. P. ..
  • A. Ramos

  - ORGANIC & BIOMOLECULAR CHEMISTRY - Year 2012

  Based on the benzo[b]naphtho[1,2-d]furan and benzo[b]naphtho[1,2-d]thiophene frameworks, a series of ligands with different basic side chains (BSCs) has been synthesized and pharmacologically evaluated. Also, their binding modes have been modelled using docking techniques. It was found that the introduction of a BSC in these systems brings about a decrease of affinity for both estrogen receptors α and β in an in vitro competitive...

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• Phosphate tricyclic coumarin analogs as steroid sulfatase inhibitors: synthesis and biological activity.

  Publication

  • W. Kozak
  • M. Daśko
  • M. Masłyk
  • J. S. Pieczykolan
  • B. Gielniewski
  • J. Rachoń
  • S. Demkowicz

  - RSC Advances - Year 2014

  In the present work, we report convenient methods for the synthesis and biological evaluation of phosphate tricyclic coumarin derivatives as potential steroid sulfatase inhibitors. The described synthesis includes the straightforward preparation of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c]chromen-6-one modified...

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