Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Vincent J. Kalish"'
Autor:
Kevin J. Tomaselli, Julia Herrmann, Robert O. Sayers, Joe C. Wu, Lalitha Kodandapani, Kathy G. Jahangiri, Craig D. Fisher, David T. Winn, Edward D. Robinson, Steven P. Meduna, Robert J. Ternansky, Pauline Yeo, Karen L. Valentino, Jose-Luis Diaz, Vincent J. Kalish, Steven D. Linton, Kristen Sebring, Robert A. Armstrong, Joseph F. Krebs, Niel C. Hoglen, Alfred P. Spada, Brad P. Hirakawa, Ning Chen, Brett R. Ullman, Brett Weylan Ching, Cheng-zhi Zhang, Xu Bai, Xin Gu, Kip Nalley, Long-Shiuh Chen, Patricia L. Gladstone, Jeff McQuiston, Teresa Aja, Todd Groessl, Donald S. Karanewsky, Suzanne Weeks, Lawrence C. Fritz, Patricia C. Contreras
Publikováno v:
Journal of Medicinal Chemistry. 48:6779-6782
A series of oxamyl dipeptides were optimized for pan caspase inhibition, anti-apoptotic cellular activity and in vivo efficacy. This structure-activity relationship study focused on the P4 oxamides and warhead moieties. Primarily on the basis of in v
Autor:
Edward D. Robinson, Silvio Roggo, Joe C. Wu, Robert J. Ternansky, Jose-Luis Diaz, Teresa Aja, Kevin J. Tomaselli, Steven P. Meduna, Vincent J. Kalish, Donald S. Karanewsky, Robert O. Sayers, Albert Schmitz, Brett R. Ullman, Julia Herrmann, Kip Nalley, Thomas L. Deckwerth
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3623-3626
Various aryloxy methyl ketones of the 1-naphthyloxyacetyl-Val-Asp backbone have been prepared. A systematic study of their structure-activity relationship (SAR) related to caspases 1, 3, 6, and 8 is reported. Highly potent irreversible broad-spectrum
Autor:
S. D. Hatch, Mark A. Muesing, Deborah A. Khalil, Nickolay Y. Chirgadze, Siegfried H. Reich, Vincent J. Kalish, Kenneth S. Su, Jeffrey A. Burgess, Krzysztof Appelt, Bruce A. Dressman, Penny P. Lubbehusen, Stephen W. Kaldor, Bhasker V. Shetty, Kristina M. Campanale, Jay F. Davies, David K. Clawson, John H. Tatlock, Maha B. Kosa, James E. Fritz, Amy K. Patick
Publikováno v:
Journal of Medicinal Chemistry. 40:3979-3985
Using a combination of iterative structure-based design and an analysis of oral pharmacokinetics and antiviral activity, AG1343 (Viracept, nelfinavir mesylate), a nonpeptidic inhibitor of HIV-1 protease, was identified. AG1343 is a potent enzyme inhi
Autor:
J. V. French, Richard E. Showalter, Hans E. Parge, Vincent J. Kalish, Daniel R. Knighton, John H. Tatlock, Christina T. Lewis, J. Ernest Villafranca
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:2489-2494
The preparation and evaluation of potent small molecule inhibitors of FKBP-12 rotamase activity is described. These ligands contain many of the structural features of the FK506 pyranose ring region, yet are synthetically more accessible. The versatil
Autor:
Vincent J. Kalish, Krzysztof Appelt, Jay F. Davies, Mark J. Pino, B.‐W. Wu, Stephen W. Kaldor, Dzuy Nyugen, L. Musick, Bruce A. Dressman, John H. Tatlock, Reich Siegfried Heinz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:727-732
The cocrystal structures of LY289612 and LY297135 were used as a starting point in the design of nonpeptidic HIV-1 protease inhibitors. This report details the discovery of a series of novel aromatic P 2 replacement groups. The 3-hydroxy-2-methyl ben
Autor:
Kevin A. Babiak, Vincent J. Kalish, Robert L. Shone, John H. Dygos, Mclaughlin Kathleen T, James R. Behling, John S. Ng, Steven W. Kramer
Publikováno v:
ChemInform. 22
Autor:
R. E. Showalter, Vincent J. Kalish, John H. Tatlock, Jesus Ernesto Villafranca, J. V. French, Daniel R. Knighton, Hans E. Parge, C. T. Lewis
Publikováno v:
ChemInform. 27
Autor:
Vincent J. Kalish, Tays Kevin L, Larisa Serdyuk, Ge Xiao, Jie Zhang, Dana Ferraris, Susan Lautar, Weixing Li, Jia-He Li, Paul W. Kletzly
Publikováno v:
ChemInform. 32
1-, 2-, 3-, 4-, 8-, or 10-Substituted 5(H)phenanthridin-6-ones were synthesized and found to be potent PARP1 inhibitors. Among the 28 compounds prepared, some showed not only low IC50 values (compound 1b, 10 nM) but also desirable water solubility ch
Publikováno v:
The Journal of Organic Chemistry. 55:105-111
La methode presentee s'effectue a partir du bromo-2 ethylenedioxy-3 norbornanecarboxylate-7 de methyle; elle conduit uniquement au dihydro-4a,7a methoxy-1 cyclopenta [c] pyrannedicarboxylate-3,5 de methyle
Publikováno v:
Tetrahedron. 46:8067-8074
The carbon framework for carbapenems was constructed by an asymmetric aldol condensation and subsequent direct coupling of the resulting β-hydroxy acid equivalent with an aminophosphonoacetate. Cyclization to the monocyclic β-lactam 20 was followed