Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Roy L. Harris"'
Autor:
Courtney G. Havens, Correa Matthew D, Rama K. Narla, Frans Baculi, Kercher Timothy S, Thomas O. Daniel, Roy L. Harris, Brian E. Cathers, Matt Alexander, Mehran F. Moghaddam, Grant Virginia Heather Sharron, Veronique Plantevin, James Carmichael, Katalin Ebinger, Antonia Lopez-Girona, Gody Khambatta, Derek Mendy, Lawrence G Hamann, Joshua Hansen, Katerina Leftheris, Brandon Wade Whitefield, Joseph Piccotti, Nagy Mark A, Rupert Vessey, Yang Tang, Laurie LeBrun, Jim Leisten, Dehua Huang
Publikováno v:
Journal of Medicinal Chemistry. 63:6648-6676
Many patients with multiple myeloma (MM) initially respond to treatment with modern combination regimens including immunomodulatory agents (lenalidomide and pomalidomide) and proteasome inhibitors. However, some patients lack an initial response to t
Autor:
Sogole Bahmanyar, Brian E. Cathers, Mehran F. Moghaddam, Peter Worland, Lida Tehrani, Brandon Wade Whitefield, Heather Raymon, James C. Gamez, Godrej Khambatta, Julius Apuy, Samantha J. Richardson, Rene R. Bisonette, Jingjing Zhao, Graziella I. Shevlin, Deborah Mortensen, Matt Hickman, Jan Elsner, Correa Matthew D, Roy L. Harris, Sophie Perrin-Ninkovic, Rama K. Narla, Jennifer Riggs, Kimberly Elizabeth Fultz, Sabita Sankar, Patrick Papa, John Sapienza, Stacie S. Canan, Sophie X. Peng, Jason Simon Parnes, Garrick Packard, Jim Leisten, Branden Lee
Publikováno v:
Journal of Medicinal Chemistry. 58:5599-5608
We report here the synthesis and structure-activity relationship (SAR) of a novel series of triazole containing mammalian target of rapamycin (mTOR) kinase inhibitors. SAR studies examining the potency, selectivity, and PK parameters for a series of
Autor:
Jason Simon Parnes, Rene R. Bisonette, Sophie Perrin-Ninkovic, Deborah Mortensen, Branden Lee, Peter Worland, James C. Gamez, Graziella I. Shevlin, Matt Hickman, Stacie S. Canan, Julius Apuy, Samantha J. Richardson, Jingjing Zhao, Godrej Khambatta, Sophie X. Peng, Jim Leisten, Garrick Packard, Correa Matthew D, Rama K. Narla, Lida Tehrani, Jennifer Riggs, Heather Raymon, Jan Elsner, Roy L. Harris, Kimberly Elizabeth Fultz, Patrick Papa, Sogole Bahmanyar, Brandon Wade Whitefield, Sabita Sankar, John Sapienza, Mehran F. Moghaddam, Brian E. Cathers
Publikováno v:
Journal of Medicinal Chemistry. 58:5323-5333
We report here the synthesis and structure-activity relationship (SAR) of a novel series of mammalian target of rapamycin (mTOR) kinase inhibitors. A series of 4,6- or 1,7-disubstituted-3,4-dihydropyrazino[2,3-b]pyrazine-2(1H)-ones were optimized for
Autor:
Sabita Sankar, Matt Hickman, Roy L. Harris, Rene R. Bisonette, Gody Khambatta, Deborah Mortensen, Kimberly Elizabeth Fultz, Sophie Perrin-Ninkovic, Branden Lee, Graziella I. Shevlin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6793-6799
We report here the discovery of a novel series of selective mTOR kinase inhibitors. A series of imidazo[4,5-b]pyrazin-2-ones, represented by screening hit 1, was developed into lead compounds with excellent mTOR potency and exquisite kinase selectivi
Autor:
Matt Hickman, Sophie X. Peng, Graziella I. Shevlin, Rama K. Narla, Jim Leisten, Rene R. Bisonette, Sophie Perrin-Ninkovic, Deborah Mortensen, Branden Lee, Gody Khambatta, Jim Gamez, Brandon Wade Whitefield, Sabita Sankar, John Sapienza, Jason Simon Parnes, Roy L. Harris, Kimberly Elizabeth Fultz
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(6)
We report here the discovery of a novel series of selective mTOR kinase inhibitors and the identification of CC214-2, a compound with demonstrated anti-tumor activity upon oral dosing in a PC3 prostate cancer xenograft model. A series of 4,6-disubsti
Autor:
Dan Zhu, Margaret A. Mccarrick, Tam Tran, Jason Katz, Graziella I. Shevlin, Roy L. Harris, Paul Erdman, Samantha J. Richardson, Yuedi W. Fleming, April Bai, Garrick Packard, Lida Tehrani, Robert Hilgraf, Jim Leisten, Yang Tang, Sakata Steven T, Brian E. Cathers, Patrick Papa, Mehran F. Moghaddam, Sophie Perrin-Ninkovic, Dale Robinson, Jennifer Riggs
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(1)
The serine/threonine specific protein kinase B-Raf is part of the MAPK pathway and is an interesting oncology target. We have identified thieno[2,3-d]pyrimidines as a core scaffold of small molecule B-Raf inhibitors. The SAR of analogs in this series
Autor:
Jennifer Riggs, Patrick Papa, Ronald Albers, Sabita Sankar, John Sapienza, Roy L. Harris, Branden Lee, Peter Worland, Mercedes Delgado, Christine Kang, Deborah Mortensen, Sophie Perrin-Ninkovic, Weiming Xu
Publikováno v:
Blood. 112:1579-1579
Mantle cell lymphoma (MCL) is a distinct sub-type non-Hodgkin lymphoma characterized by overexpression of cyclin D1 (CCND1) in 95% of patients due to the cytogenetic change of chromosome translocation t(11;14) (q13;q32). It remains one of the most ch