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Publikováno v:
Journal of Hypertension
Context: We describe the clinical investigation of the first generation aldosterone synthase inhibitor, LCI699, in patients with essential, uncontrolled, resistant, or secondary hypertension. LCI699 competitively reduced blood pressure at lower doses
Autor:
Kenneth S. Leonards, Steele Ronald Edward, Jong M. Wasvary, E.C. Yurachek, Zouhair F. Stephan, Chii Whei Hu, Robin Sharif, Thomas H. Hintze
Publikováno v:
Atherosclerosis. 126:53-63
A potent lipid-lowering thyromimetic (CGS 26214) devoid of cardiac and thermogenic activity was identified based on its ability to preferentially access and bind the nuclear fraction of hepatocytes over that of myocytes in culture. The difference in
Publikováno v:
ChemInform. 22
A new class of potent, selective, nonsteroidal inhibitors of aromatase have been discovered. The most potent member of this series is fadrozole hydrochloride, CGS 16949 A, 4-(5,6,7,8-tetrahydroimidazo[1,5-alpha]pyridin-5-yl)benzonitrile monohydrochlo
Autor:
Colin Howes, Jong M. Wasvary, Zouhair F. Stephan, Steele Ronald Edward, E.C. Yurachek, Robin Sharif
Publikováno v:
Biochemical Pharmacology. 43:1969-1974
This study was designed to determine whether the conjugation product of L-T3 with cholic acid would result in a liver-targeted compound (CGH 509A) with hypocholesterolemic (HC) activity significantly dissociable from cardiovascular (CV) and thyroxine
Publikováno v:
Journal of Medicinal Chemistry. 34:725-736
A new class of potent, selective, nonsteroidal inhibitors of aromatase have been discovered. The most potent member of this series is fadrozole hydrochloride, CGS 16949 A, 4-(5,6,7,8-tetrahydroimidazo[1,5-alpha]pyridin-5-yl)benzonitrile monohydrochlo
Autor:
Steele Ronald Edward, Ajay S. Bhatnagar, Klaus Schieweck, Leslie J. Browne, Bowman Robert M, A. Häusler
Publikováno v:
The Journal of Steroid Biochemistry and Molecular Biology. 37:363-367
Aminoglutethimide (AG), an inhibitor of the aromatase enzyme, inhibits the biosynthesis of estrogens and displays well-documented anti-tumor efficacy in breast-cancer. However, this efficacy is accompanied by a relative lack of specificity in inhibit
Autor:
Steele Ronald Edward, Ricardo E. Chatelain, Wendy D. Cornell, Christian Honer, Gary Michael Ksander, Robert Schweitzer, Kiyean Nam, Marshall Paul James, Christoph Schumacher, Cynthia A. Fink
Publikováno v:
Molecular pharmacology. 63(5)
The steroid compound cyproterone acetate was identified in a high-throughput screen for glucocorticoid receptor (GR) binding compounds. Cyproterone (Schering AG) is clinically used as an antiandrogen for inoperable prostate cancer, virilizing syndrom
Autor:
David Louis Feldman, Randy L. Webb, Warren Lee, Ashok Hospattankar, Michael Jeune, Alan D. Neubert, Natalie A. Bilci, Natalya Alexander, Andrew M. Yuan, Therese C Mogelesky, Aida E. Navarrete, Gary Michael Ksander, Joyce C. Gibson, Eric Carlson, Haamid M. Sharif, Eli M. Wallace, Jong Wasvery, Reynalda Dejesus, Paivi Jaana Kukkola, Edna Cahill, Michael A. Moskal, Cynthia A. Fink, Steele Ronald Edward, Zouhair F. Stephan, Kevin Poirier
Publikováno v:
Journal of medicinal chemistry. 44(26)
The synthesis and biological activities of biarylamide-substituted diaminoindanes as microsomal triglyceride transfer protein (MTP) inhibitors are described. One of the more potent compounds, 8aR, inhibited both the secretion of apoB from Hep G2 cell
Autor:
Zouhair F. Stephan, Ronald Dotson, Steele Ronald Edward, Jong M. Wasvary, Edna Cahill, Hollis C. Tomaselli, James L. Stanton, Jenny Tan
Publikováno v:
ChemInform. 31
The synthesis of substituted phenoxyphenyl oxamic acid derivatives related to l -thyronine ( l -T3) is described. The in vitro and in vivo cholesterol lowering and cardiovascular effects of these compounds are presented and discussed.