Molecules

Synthesis and Biological Evaluation of Thieno [3, 2-d]-pyrimidinones, Thieno [3, 2-d] pyrimidines and Quinazolinones: Conformationally Restricted 17b- …

E Perspicace, S Marchais-Oberwinkler, RW Hartmann

Index: Perspicace, Enrico; Marchais-Oberwinkler, Sandrine; Hartmann, Rolf W. Molecules, 2013 , vol. 18, # 4 p. 4487 - 4509

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Citation Number: 3

Abstract

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 17β-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 ...