Synthesis and biological evaluation of thieno[3,2-d]- pyrimidinones, thieno[3,2-d]pyrimidines and quinazolinones: conformationally restricted 17b-hydroxysteroid dehydrogenase type 2 (17b-HSD2) inhibitors.
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AbstractIn this study, a series of conformationally restricted thieno[3,2-d]pyrimidinones, thieno[3,2-d]pyrimidines and quinazolinones was designed and synthesized with the goal of improving the biological activity as 17b-hydroxysteroid dehydrogenase type 2 inhibitors of the corresponding amidothiophene derivatives. Two moderately active compounds were discovered and this allowed the identification of the biologically active open conformer as well as the extension of the enzyme binding site characterisation.
CitationSynthesis and biological evaluation of thieno[3,2-d]- pyrimidinones, thieno[3,2-d]pyrimidines and quinazolinones: conformationally restricted 17b-hydroxysteroid dehydrogenase type 2 (17b-HSD2) inhibitors. 2013, 18 (4):4487-509 Molecules
AffiliationPharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany.
JournalMolecules (Basel, Switzerland)
The following license files are associated with this item:
- Synthesis and biological evaluation of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors based on a thieno[2,3-d]pyrimidin-4(3H)-one core.
- Authors: Lilienkampf A, Karkola S, Alho-Richmond S, Koskimies P, Johansson N, Huhtinen K, Vihko K, Wähälä K
- Issue date: 2009 Nov 12
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- Issue date: 2008 Mar
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- Issue date: 2001 Aug 2
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- Issue date: 2012 Sep 1
- Synthesis and 3 alpha-hydroxysteroid dehydrogenase inhibitory activity of some N(6)-(pyrazol-5-yl)-pyr-azolo[4,3-d]pyrimidin-7-ones.
- Authors: Migliara O, Plescia S, Schillaci D
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