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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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.

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 ...

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3b-Hydroxysteroid Dehydrogenase/D-Isomerase Activity Associated with the Human 17b-Hydroxysteroid Dehydrogenase Type 2 Isoform*

The type 2 isoform of human 17b-hydroxysteroid dehydrogenase (17bHSD2) efficiently catalyzes the oxidative metabolism of androgens and estrogens, and it is expressed in a large series of human peripheral tissues. To obtain a better understanding of the regulation of local steroid biosynthesis and metabolism in human tissues, we have established a dual steroidogenic activity of the 17bHSD2 enzym...

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Synthesis and biological evaluation of conformationally restricted adenine bicycloribonucleosides.

We prepared a novel series of conformationally restricted bicyclonucleosides and nucleotides. The synthetic approach employed a ring closing metathesis to provide access to both 6 and 7 membered saturated and unsaturated rings linking the 3' to 5' methylene groups of the sugar. The bicyclonucleosides were also transformed to the corresponding phosphoramidate prodrugs by an innovative one-pot pr...

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Synthesis and Molecular Docking Studies of 2-arylideneindan-1,3-diones Derivatives as an Inhibitor of 17β-hydroxysteroid Dehydrogenase Type 1

Due to the drawbacks of applying catalysts in the synthesis of α,β-unsaturated structure units and the importance of these materials, electrochemistry has been introduced as an efficient alternative.Therefore, herein a high-yield synthesis of 2-arylideneindan-1,3-diones is proposed. The procedure is carried out in propanol, using electrons as a green catalyst for generating propanol anion...

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Expression and Characterization of Recombinant Type 2 3a- Hydroxysteroid Dehydrogenase (HSD) from Human Prostate: Demonstration of Bifunctional 3a/17b-HSD Activity and Cellular Distribution

In androgen target tissues, 3a-hydroxysteroid dehydrogenase (3a-HSD) may regulate occupancy of the androgen receptor (AR) by catalyzing the interconversion of 5a-dihydrotestosterone (5a-DHT) (a potent androgen) and 3a-androstanediol (a weak androgen). In this study, a 3a-HSD cDNA (1170 bp) was isolated from a human prostate cDNA library. The human prostatic 3a-HSD cDNA encodes a 323amino acid p...

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ژورنال

عنوان ژورنال: Molecules

سال: 2013

ISSN: 1420-3049

DOI: 10.3390/molecules18044487