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.

2.50
Hdl Handle:
http://hdl.handle.net/10033/299504
Title:
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.
Authors:
Perspicace, Enrico; Marchais-Oberwinkler, Sandrine; Hartmann, Rolf W
Abstract:
In 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.
Affiliation:
Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany.
Citation:
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. 2013, 18 (4):4487-509 Molecules
Journal:
Molecules (Basel, Switzerland)
Issue Date:
2013
URI:
http://hdl.handle.net/10033/299504
DOI:
10.3390/molecules18044487
PubMed ID:
23591928
Type:
Article
Language:
en
ISSN:
1420-3049
Appears in Collections:
publications of the department drug design and optimization (HIPS]DDOP)

Full metadata record

DC FieldValue Language
dc.contributor.authorPerspicace, Enricoen_GB
dc.contributor.authorMarchais-Oberwinkler, Sandrineen_GB
dc.contributor.authorHartmann, Rolf Wen_GB
dc.date.accessioned2013-08-22T12:14:57Z-
dc.date.available2013-08-22T12:14:57Z-
dc.date.issued2013-
dc.identifier.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 Moleculesen_GB
dc.identifier.issn1420-3049-
dc.identifier.pmid23591928-
dc.identifier.doi10.3390/molecules18044487-
dc.identifier.urihttp://hdl.handle.net/10033/299504-
dc.description.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.en_GB
dc.language.isoenen
dc.rightsArchived with thanks to Molecules (Basel, Switzerland)en_GB
dc.titleSynthesis 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.en
dc.typeArticleen
dc.contributor.departmentPharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany.en_GB
dc.identifier.journalMolecules (Basel, Switzerland)en_GB

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