Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Hwa-Kwo Yen"'
Autor:
Martin Brandt, Andrew D. Abell, Mark Alan Levy, Dennis A. Holt, Dennis S. Yamashita, Hwa-Kwo Yen, Karl F. Erhard, Hadiza Mohammed
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:1365-1368
A preparative chiral HPLC separation of each of the four stereoisomers of LY191704 [(±)-1, and (±)-3] and LY266111 [(±)-2, and (±)-4] is reported. All eight compounds have been evaluated in vitro as inhibitors of recombinant human type 1 and type
Autor:
Mary J. Bossard, Arnold J. Krog, Hwa-Kwo Yen, Karl F. Erhard, Arda Konialian-Beck, Elizabeth Ortiz, Hye-Ja Oh, Martin Brandt, Mark Alan Levy, Dennis A. Holt, Juan I. Luengo, Leonard W. Rozamus
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:315-320
A series of non-macrocyclic pipecolyl α-ketoamides were prepared and evaluated as FKBP cis-trans peptidyl-prolyl isomerase inhibitors. These compounds exhibited inhibition constants as low as 2 nM. Their design was based on a consideration of the co
Autor:
Dennis A. Holt, Juan I. Luengo, Dennis S. Yamashita, Hye Ja Oh, Arda L. Konialian, Hwa Kwo Yen, Leonard W. Rozamus, Martin Brandt, Mary J. Bossard, Mark A. Levy, Drake S. Eggleston, Jun Liang, L. Wayne Schultz, Thomas J. Stout, Jon Clardy
Publikováno v:
Journal of the American Chemical Society. 115:9925-9938
Autor:
W Metcalf Brian, Martin Brandt, Mark Alan Levy, Hye-Ja Oh, Dennis A. Holt, Hwa-Kwo Yen, Leonard W. Rozamus
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:1735-1738
A series of 3-carboxymethyl steroids has been prepared and assayed in vitro as inhibitors of steroid 5α-reductase isolated from human prostatic tissue. Potent inhibition was observed with analogs from both androstene and estratriene families. Phosph
Autor:
Jill M. Erb, Martin Brandt, Hye-Ja Oh, Dennis A. Holt, Brian W. Metcalf, Hwa-Kwo Yen, Leonard W. Rozamus, Mark Alan Levy, Julie I. Heaslip
Publikováno v:
Bioorganic Chemistry. 19:245-260
3-Phosphinic acid and 3-phosphonic acid steroids are presented as a new class of steroid 5α-reductase (SR) inhibitors. Representative compounds have been studied as inhibitors of prostatic SR from human, rat, and cynomolgus monkey ( Macaca fascicula
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 1:27-32
A series of A-ring unsaturated 3-nitrosteroids has been prepared and assayed in vitro as inhibitors of steroid 5α-reductase. One of these compounds, 3-nitro-5α-androst-3-ene-17β-diisopropylcarboxamide (4), inhibits the human enzyme with a Ki of 50
Autor:
Jian Li, Harold R. Almond, Steven A. Middleton, Dana L. Johnson, Gregory C. Leo, Donald Ludovici, Judith Baker, Stuart Emanuel, Hwa-Kwo Yen, Robert A. Galemmo, Robert H. Gruninger, Eric D. Strobel, Ann Devine, Rose Tominovich, Chih Y. Ho, Laura Andraka, Jay Mei, Hong Lu, Umar Maharoof, Robert W. Tuman, Jan L. Sechler
Publikováno v:
Journal of medicinal chemistry. 48(26)
A series of (6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines has been optimized to preserve both potent kinase inhibition activity against the angiogenesis target, the receptor tyrosine kinase of Platelet-Derived Growth Factor-BB (PDG
Autor:
Dinu Shah, Dennis S. Yamashita, Martin Brandt, Hwa-Kwo Yen, Mark Alan Levy, Dennis A. Holt, Hye-Ja Oh
Publikováno v:
Bioorganicmedicinal chemistry. 4(9)
Steroidal 3-carboxy-20-ketones have been prepared within two structural series, the androsta-3,5-dienes and the estra-1,3,5-trienes, as potential inhibitors of types 1 and 2 steroid 5α-reductase, the enzyme activity responsible for the final step in
Publikováno v:
The Journal of Organic Chemistry. 49:4595-4601
Synthese d'acyl- et benzenesulfonyl-3 isoxazolines-2 (A) par cycloaddition de composes ethyleniques et d'esters de methyle d'acyl- et benzenesulfonyl acinitromethanes; transformations des composes A
Autor:
Leonard W. Rozamus, Juan I. Luengo, Richard Heys, Annalisa Hand, Randall K. Johnson, Arthur Shu, Damien J. Dunnington, Karla D'Alessio, Polongpon Kongsaeree, Dennis A. Holt, Hwa-Kwo Yen, Tonie Newman-Tarr, Terence Porter, Jon Clardy, Mark Alan Levy, Jungwon Choi, Dennis S. Yamashita, Alison Badger, Mary J. Bossard, Arda Konialian Beck, Leo F. Faucette
Publikováno v:
Chemistry & Biology. (7):471-481
Background : Rapamycin is an immunosuppressant natural product, which blocks T -cell mitogenesis and yeast proliferation. In the cytoplasm, rapamycin binds to the immunophilin FKBP12 and the complex of these two molecules binds to a recently discover