Journal
COMPTES RENDUS CHIMIE
Volume 12, Issue 10-11, Pages 1117-1126Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.crci.2009.03.007
Keywords
Steroidogenic CYP enzymes; Substructure combination approach; Inhibitors; Drug targets; Breast cancer; Prostate cancer; Congestive heart failure
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Funding
- European Postgraduate School [532]
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Four out of six CYP enzymes involved in steroid biosynthesis are very interesting targets for the development of new drugs in order to treat a variety of severe illnesses. Herein we report on a novel approach for the discovery of hit compounds using new combinations of substructures of known CYP inhibitors. The synthesis of new scaffolds and their biological evaluation regarding inhibition of CYP17, CYP19, CYP11B1 and CYP11B2 are described. Thus, the very active (IC50 = 114 and 100 nM) and selective (IC50 > 1000 nM) CYP11B2 inhibitors, compounds 4 and 5, were obtained as well as the dual inhibitor 3, reducing the activities of CYP19 and CYP11B2. To cite this article: Ulrike E. Hille et al., C R. Chimie 12 2009. (C) 2009 Academie des sciences. Published by Elsevier Masson SAS. All rights reserved.
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