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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

1
,
1
 and
1,2,*
Received: 22 March 2013 / Revised: 8 April 2013 / Accepted: 10 April 2013 / Published: 16 April 2013
(This article belongs to the Section Medicinal Chemistry)
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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 thieno[3,2-d]pyrimidinones; thieno[3,2-d]pyrimidines; quinazolinones; conformationally restricted analogues; enzyme inhibitors; 17b-hydroxysteroid dehydrogenase type 2; osteoporosis
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.

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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.

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