Zobrazeno 1 - 3
of 3
pro vyhledávání: '"Kevin J. Curran"'
Autor:
Arie Zask, Lourdes Toral-Barza, Jeroen C. Verheijen, Natasja Brooijmans, David J. Richard, Semiramis Ayral-Kaloustian, Ker Yu, Kevin J. Curran, Joshua Kaplan, Irwin Hollander, Eric M. Bennett
Publikováno v:
Journal of Medicinal Chemistry. 52:7942-7945
Dramatic improvements in mTOR-targeting selectivity were achieved by replacing morpholine in pyrazolopyrimidine inhibitors with bridged morpholines. Analogues with subnanomolar mTOR IC(50) values and up to 26000-fold selectivity versus PI3Kalpha were
Autor:
Kevin J. Curran, Boris Feld, Amar S. Prashad, Anita Y. M. Howe, John O'Connell, Martin Joseph Digrandi, Atul Agarwal, Alan G. Sutherland, Bloom Jonathan David, Bernard Dean Johnson, Thomas Nittoli, Shabana Insaf, Rajiv Chopra, Mark Orlowski, Karen L. Wheless, M. Brawner Floyd, Tarek S. Mansour
Publikováno v:
Journal of Medicinal Chemistry. 50:2108-2116
A series of potent anthranilic acid-based inhibitors of the hepatitis C NS5B polymerase has been identified. The inhibitors bind to a site on NS5B between the thumb and palm regions adjacent to the active site as determined by X-ray crystallography o
Autor:
John O'Connell, Kevin J. Curran, Kristine Svenson, Anita Y. M. Howe, Kitae Lim, Steven F. Sukits, Mengxiao Shi, Ariamala Gopalsamy, Boris Feld, Girija Krishnamurthy, Rajiv Chopra, Tarek S. Mansour, Atul Agarwal, Mark Orlowski, Joel Bard, John W. Ellingboe, Gregory Ciszewski
Publikováno v:
Journal of Medicinal Chemistry. 49:3052-3055
Through high throughput screening, substituted proline sulfonamide 6 was identified as HCV NS5b RNA-dependent RNA polymerase inhibitor. Optimization of various regions of the lead molecule resulted in compounds that displayed good potency and selecti