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

Autor: Rolf W. Hartmann, Enrico Perspicace, Sandrine Marchais-Oberwinkler
Jazyk: angličtina
Rok vydání: 2013
Předmět:
Zdroj: Molecules, Vol 18, Iss 4, Pp 4487-4509 (2013)
Druh dokumentu: article
ISSN: 1420-3049
DOI: 10.3390/molecules18044487
Popis: 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.
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