Molecules 2013, 18(4), 4487-4509; doi:10.3390/molecules18044487
Article

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

Received: 22 March 2013; in revised form: 8 April 2013 / Accepted: 10 April 2013 / Published: 16 April 2013
(This article belongs to the Section Medicinal Chemistry)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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.
Keywords: thieno[3,2-d]pyrimidinones; thieno[3,2-d]pyrimidines; quinazolinones; conformationally restricted analogues; enzyme inhibitors; 17b-hydroxysteroid dehydrogenase type 2; osteoporosis
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MDPI and ACS Style

Perspicace, E.; Marchais-Oberwinkler, S.; Hartmann, R.W. 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. Molecules 2013, 18, 4487-4509.

AMA Style

Perspicace E, Marchais-Oberwinkler S, Hartmann RW. 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. Molecules. 2013; 18(4):4487-4509.

Chicago/Turabian Style

Perspicace, Enrico; Marchais-Oberwinkler, Sandrine; Hartmann, Rolf W. 2013. "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." Molecules 18, no. 4: 4487-4509.

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