Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the …

…, S Marchais-Oberwinkler, RW Hartmann

Index: Voets, Marieke; Antes, Iris; Scherer, Christiane; Mueller-Vieira, Ursula; Biemel, Klaus; Marchais-Oberwinkler, Sandrine; Hartmann, Rolf W. Journal of Medicinal Chemistry, 2006 , vol. 49, # 7 p. 2222 - 2231

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Citation Number: 72

Abstract

In this study, the synthesis and biological evaluation of heteroaryl-substituted dihydronaphthalenes and indenes (1-16) is described. The compounds were tested for activity by use of human CYP11B2 expressed in fission yeast and V79 MZh cells and for selectivity by use of human CYP11B1, CYP17, and CYP19. The most active inhibitor was the 6-methoxydihydronaphthalene 4 (IC50= 2 nM), showing a K i value of 1.3 nM and a ...