Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Nikole Randolph"'
Autor:
Bryson Rast, Alexandre J. Buckmelter, Li Ren, Walter C. Voegtli, Greg Miknis, Robert J. Ely, Tony Morales, Guy Vigers, Nikole Randolph, Ellen R. Laird, Michele Callejo, Joseph P. Lyssikatos, Sarah Galbraith, Matthew Martinson, Stephen T. Schlachter, Barbara J. Brandhuber, Steve Wenglowsky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1243-1247
The development of inhibitors of B-Raf(V600E) serine-threonine kinase is described. Various head-groups were examined to optimize inhibitor activity and ADME properties. Several of the head-groups explored, including naphthol, phenol and hydroxyamidi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::73adb84e1114bda90d7b78517b2d0ef5
https://doi.org/10.1016/j.bmcl.2010.12.061
https://doi.org/10.1016/j.bmcl.2010.12.061
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::01679be6189825d6dd1ca0c8f7d6aab9
https://doi.org/10.1016/j.bmcl.2008.07.002
https://doi.org/10.1016/j.bmcl.2008.07.002
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7453447f90b377bcf825db60a43c00ae
https://pubmed.ncbi.nlm.nih.gov/24900315
https://pubmed.ncbi.nlm.nih.gov/24900315
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15d2ef9017c0890fcfd275c77fdaaee5
https://pubmed.ncbi.nlm.nih.gov/21536432
https://pubmed.ncbi.nlm.nih.gov/21536432
Autor:
Li Ren, Tony Morales, Matthew Martinson, Jonas Grina, Guy Vigers, Joseph P. Lyssikatos, Michele Callejo, Greg Miknis, Mike Welch, Bryson Rast, Barbara J. Brandhuber, Eugene Tarlton, Nikole Randolph, Ellen R. Laird, Stephen T. Schlachter, Steve Wenglowsky, Alexandre J. Buckmelter
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(4)
Virtual and high-throughput screening identified imidazo[1,2-a]pyrazines as inhibitors of B-Raf. We describe the rationale, SAR, and evolution of the initial hits to a series of furo[2,3-c]pyridine indanone oximes as highly potent and selective inhib
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91ecb177a764a3a1498267492422d893
https://pubmed.ncbi.nlm.nih.gov/21211972
https://pubmed.ncbi.nlm.nih.gov/21211972
Autor:
Nikole Randolph, Bin Wang, Shannon L. Winski, Gunawardana Indrani W, Ira von Carlowitz, Michael J. Humphries, Yvan Le Huerou, Lyon Michael, Eli M. Wallace, Michael L. Schrag, Jim Blake, Mark Joseph Chicarelli, Mohr Peter
Publikováno v:
Molecular Cancer Therapeutics. 8:B254-B254
Loss of coordination between cell cycle checkpoints and DNA damage repair is a fundamental feature tumor cells rely on for unregulated growth and developing chemotherapeutic resistance. The protein kinase Checkpoint kinase 1 (Chk1) is a sentinel mole
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e0445ee4e81ed409b1134de5d278d015
https://doi.org/10.1158/1535-7163.targ-09-b254
https://doi.org/10.1158/1535-7163.targ-09-b254