Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Joshua D, Hansen"'
Autor:
Joshua D, Hansen, Kevin, Condroski, Matthew, Correa, George, Muller, Hon-Wah, Man, Alexander, Ruchelman, Weihong, Zhang, Fan, Vocanson, Tim, Crea, Wei, Liu, Gang, Lu, Frans, Baculi, Laurie, LeBrun, Afshin, Mahmoudi, Gilles, Carmel, Matt, Hickman, Chin-Chun, Lu
Publikováno v:
Journal of medicinal chemistry. 61(2)
We previously disclosed the identification of cereblon modulator 3 (CC-885), with potent antitumor activity mediated through the degradation of GSPT1. We describe herein the structure-activity relationships for analogs of 3 with exploration of the st
Autor:
Victoria Dinkel, Jonas Grina, David A. Moreno, Simon Mathieu, Joshua D. Hansen, Kevin Rasor, Gregg Hastings, Walter C. Voegtli, Guy Vigers, Sumeet Rana, Joachim Rudolph, Susan L. Gloor, Ellen R. Laird, Li Ren, Steve Wenglowsky, Brandon S. Willis, Hillary L. Sturgis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1923-1927
Herein we describe the design of a novel series of ATP competitive B-Raf inhibitors via structure-based methods. These 3-N-methylquinazoline-4(3H)-one based inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. Optimizati
Autor:
Janet Gunzner-Toste, Edna F. Choo, Bruno Alicke, Stephen E. Gould, Rebecca Pulk, Ellen R. Laird, Zhaoyang Wen, Li Ren, Jonas Grina, Jason Boggs, David A. Moreno, Joachim Rudolph, Alexandre J. Buckmelter, Simon Mathieu, Guiling Zhao, Stefan Gradl, Walter C. Voegtli, Yingqing Ran, Ignacio Aliagas, Joshua D. Hansen, Georgia Hatzivassiliou, Wendy Lee, Victoria Dinkel, Steve Wenglowsky, Gregg Hastings, Susan L. Gloor
Publikováno v:
Journal of Medicinal Chemistry. 55:2869-2881
Recent clinical data provided proof-of-concept for selective B-Raf inhibitors in treatment of B-Raf(V600E) mutant melanoma. Pyrazolopyridine-type B-Raf inhibitors previously described by the authors are potent and selective but exhibit low solubility
Autor:
Barbara J. Brandhuber, George T. Topalov, Michele Callejo, Matthew Martinson, Nikole Randolph, Susan L. Gloor, Ellen R. Laird, Brad Newhouse, Mike Welch, Joseph P. Lyssikatos, Joshua D. Hansen, Jonas Grina, Rich Woessner, Alan G. Olivero, Guy Vigers, Nicole M Littman, Tony Morales
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4692-4695
Herein we describe a novel pyrazole-based class of ATP competitive B-Raf inhibitors. These inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. A subset of these inhibitors has demonstrated the ability to inhibit downstr
Autor:
Brad Newhouse, Christine D. Eberhardt, John Gaudino, Andrew Allen, C. Todd Eary, Shelley Allen, Joshua D. Hansen, Justin G. Schiro, Aaron S. Anderson, Laurence E. Burgess, Ellen R. Laird, David Chantry
Publikováno v:
Tetrahedron Letters. 47:69-72
The synthesis of racemic and non-racemic spirocyclic lactams that display high binding affinity toward CCR4 is described. Two distinct series of spirocycles were prepared from the common intermediate 9.
Autor:
Jonas Grina, David A. Moreno, Alexandre J. Buckmelter, Ellen R. Laird, Steve Wenglowsky, Li Ren, Jeongbeob Seo, Bainian Feng, Simon Mathieu, Stefan Gradl, Joachim Rudolph, Susan L. Gloor, Paul Lunghofer, Brad Newhouse, Walter C. Voegtli, Kateri A. Ahrendt, Joshua D. Hansen, Tyler Risom, Zhaoyang Wen, Hillary L. Sturgis
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(18)
Structure–activity relationships around a novel series of B-RafV600E inhibitors are reported. The enzymatic and cellular potencies of inhibitors derived from two related hinge-binding groups were compared and3-methoxypyrazolopyridine proved to be s
Autor:
Kim Malesky, Victoria Dinkel, Bruno Alicke, Hillary L. Sturgis, Simon Mathieu, Ignacio Aliagas, Sumeet Rana, Kyung Song, Brandon S. Willis, Bonnie Liu, Nikole Randolph, Yingqing Ran, Scott Savage, Wendy B. Young, Edna F. Choo, Ellen R. Laird, Steve Wenglowsky, Stephen E. Gould, Bainian Feng, Michael Shrag, Joachim Rudolph, Li Ren, Kateri A. Ahrendt, Nicholas J. Raddatz, Walter C. Voegtli, Tyler Risom, LeAnn T. Selby, Jonas Grina, Zhaoyang Wen, Susan L. Gloor, Janet Gunzner-Toste, Wen-I Wu, Alexandre J. Buckmelter, Brad Newhouse, Richard Woessner, Stefan Gross, Joshua D. Hansen, Georgia Hatzivassiliou
Publikováno v:
ACS medicinal chemistry letters. 2(5)
The V600E mutation of B-Raf kinase results in constitutive activation of the MAPK signaling pathway and is present in approximately 7% of all cancers. Using structure-based design, a novel series of pyrazolopyridine inhibitors of B-Raf(V600E) was dev
Autor:
Matthew Martinson, George T. Topalov, Michele Callejo, Mike Welch, Nikole Randolph, Rich Woessner, Joseph P. Lyssikatos, Ellen R. Laird, Guy Vigers, Sarah Galbraith, Barbara J. Brandhuber, Jonas Grina, Joshua D. Hansen, Brad Newhouse, Nicole M Littman, Alan G. Olivero, Tony Morales
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(11)
The synthesis and biological evaluation of non-oxime pyrazole based B-Raf inhibitors is reported. Several oxime replacements have been prepared and have shown excellent enzyme activity. Further optimization of fused pyrazole 2a led to compound 38, a
Autor:
James D. White, Joshua D. Hansen
Publikováno v:
ChemInform. 33
A synthesis of (-)-epicylindrospermopsin (2) was completed that establishes its absolute configuration and corroborates the corrected structural assignment previously made to this toxin by Weinreb et al. The hydroxylamine 3, prepared from 4-bromobenz
Autor:
James D. White, Joshua D. Hansen
Publikováno v:
ChemInform. 36