Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Deborah Choquette"'
Autor:
Steven M. Mennen, Harikrishna Muppalla, Athimoolam Arunachalampillai, Krishna Sheena, Deborah Choquette
Publikováno v:
Synlett. 28:2330-2334
A simple five-step process for the conversion of technical grade (+)-3-carene into 6,6-dimethylbicyclo[3.1.0]hexan-3-one was developed. A robust process was required that delivered the 6,6-dimethylbicyclo[3.1.0]hexan-3-one, minimized chromatography,
Autor:
Karen Rex, Douglas A. Whittington, David Bauer, Steven F. Bellon, Jean-Christophe Harmange, Martin A. Broome, Alessandro Boezio, Christiane Boezio, Karina R. Vaida, Deborah Choquette, Isabelle Dussault, Katrina W. Copeland, Emily A. Peterson, Yohannes Teffera, Roman Shimanovich, Brian K. Albrecht, Richard T. Lewis, Michele Potashman, Jingzhou Liu, Julia Lohman, Angela Coxon, Min-Hwa Jasmine Lin, Satoko Hirai
Publikováno v:
Journal of Medicinal Chemistry. 59:2328-2342
Deregulation of the receptor tyrosine kinase mesenchymal epithelial transition factor (MET) has been implicated in several human cancers and is an attractive target for small molecule drug discovery. Herein, we report the discovery of compound 23 (AM
Autor:
Alessandro A, Boezio, Katrina W, Copeland, Karen, Rex, Brian, K Albrecht, David, Bauer, Steven F, Bellon, Christiane, Boezio, Martin A, Broome, Deborah, Choquette, Angela, Coxon, Isabelle, Dussault, Satoko, Hirai, Richard, Lewis, Min-Hwa Jasmine, Lin, Julia, Lohman, Jingzhou, Liu, Emily A, Peterson, Michele, Potashman, Roman, Shimanovich, Yohannes, Teffera, Douglas A, Whittington, Karina R, Vaida, Jean-Christophe, Harmange
Publikováno v:
Journal of medicinal chemistry. 59(6)
Deregulation of the receptor tyrosine kinase mesenchymal epithelial transition factor (MET) has been implicated in several human cancers and is an attractive target for small molecule drug discovery. Herein, we report the discovery of compound 23 (AM
Autor:
Christiane M, Bode, Alessandro A, Boezio, Brian K, Albrecht, Steven F, Bellon, Loren, Berry, Martin A, Broome, Deborah, Choquette, Isabelle, Dussault, Richard T, Lewis, Min-Hwa Jasmine, Lin, Karen, Rex, Douglas A, Whittington, Yajing, Yang, Jean-Christophe, Harmange
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4089-4093
Deregulation of the receptor tyrosine kinase c-Met has been implicated in several human cancers and is an attractive target for small molecule drug discovery. Herein, we report the discovery of a structurally diverse series of carbon-linked quinoline
Autor:
Diane M. Boucher, George Huang, Edward D. Ball, Guanjing Chen, David K. Heidary, Mark N. Namchuk, Jianguo Ma, Yung-Mae Yao, Jinwang Xu, Ron Grey, Forster Cornelia J, Greg Henkel, Jie-Hua Zhou, Michael J. Arnost, Robert J. Davies, Deborah Choquette
Publikováno v:
Journal of Medicinal Chemistry. 55:725-734
In acute myelogenous leukemia (AML), the FLT3 receptor tyrosine kinase (RTK) is highly expressed with 30% of patients expressing a mutated, constitutively active form of this protein. To inhibit this receptor, VX-322 was developed and found to be ver
Autor:
Min-Hwa Jasmine Lin, Zhiyang Zhao, Jingzhou Liu, L. Steven Hollis, Adria E. Colletti, Yohannes Teffera, Deborah Choquette
Publikováno v:
Chemical Research in Toxicology. 23:1743-1752
Compound 1, (7-methoxy-N-((6-(3-methylisothiazol-5-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)-1,5-naphthyridin-4-amine) is a potent, selective inhibitor of c-Met (mesenchymal-epithelial transition factor), a receptor tyrosine kinase that is oft
Autor:
Alessandro A, Boezio, Loren, Berry, Brian K, Albrecht, David, Bauer, Steven F, Bellon, Christiane, Bode, April, Chen, Deborah, Choquette, Isabelle, Dussault, Mei, Fang, Satoko, Hirai, Paula, Kaplan-Lefko, Jay F, Larrow, Min-Hwa Jasmine, Lin, Julia, Lohman, Michele H, Potashman, Yusheng, Qu, Karen, Rex, Michael, Santostefano, Kavita, Shah, Roman, Shimanovich, Stephanie K, Springer, Yohannes, Teffera, Yajing, Yang, Yihong, Zhang, Jean-Christophe, Harmange
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6307-6312
Deregulation of the receptor tyrosine kinase c-Met has been implicated in several human cancers and is an attractive target for small molecule drug discovery. We previously showed that O-linked triazolopyridazines can be potent inhibitors of c-Met. H
Autor:
Steven F. Bellon, Monica Reese, Jay Larrow, Isabelle Dussault, Stephanie Springer, Paula Kaplan-Lefko, Jodi Moriguchi, David Bauer, Yajing Yang, Kavita Shah, Loren Berry, Jean-Christophe Harmange, Christiane Bode, Karen Rex, Brian K. Albrecht, Yihong Zhang, Doug Hoffman, Jasmine Lin, Deborah Choquette, Alessandro Boezio, Alexander M. Long, Roman Shimanovich, Anne B. O’Connor, Aaron C. Siegmund, April Chen, Cary Fridrich, Julia Lohman, Yohannes Teffera, Michele Potashman, Satoko Hirai
Publikováno v:
Journal of Medicinal Chemistry. 51:2879-2882
Tumorigenesis is a multistep process in which oncogenes play a key role in tumor formation, growth, and maintenance. MET was discovered as an oncogene that is activated by its ligand, hepatocyte growth factor. Deregulated signaling in the c-Met pathw
Autor:
Virginia Berry, Alexander M. Long, Tom DeMelfi, Nicholas Doerr, Philip Roveto, Yohannes Teffera, Loren Berry, Anthony Polverino, Danlin Chen, Juan Estrada, George Borg, Roger Zanon, Charlie Starnes, James Bready, Shawn Harriman, Kelly Regal, Michael Schrag, Jean-Christophe Harmange, David Bauer, Russell Graceffa, Daniel S. La, Vinod F. Patel, Sesha Neervannan, Matthew Weiss, Angela Coxon, Andrew Tasker, Douglas A. Whittington, Michele Potashman, Julie Flynn, Stephen Kaufman, Deborah Choquette
Publikováno v:
Journal of Medicinal Chemistry. 51:1668-1680
We have previously shown N-arylnaphthamides can be potent inhibitors of vascular endothelial growth factor receptors (VEGFRs). N-Alkyl and N-unsubstituted naphthamides were prepared and found to yield nanomolar inhibitors of VEGFR-2 (KDR) with an imp
Autor:
Martin A. Broome, Jean-Christophe Harmange, Jodi Moriguchi, Hue T. Kha, Benny Amore, Michael A. Damore, Robert Radinsky, Richard Kendall, Teresa L. Burgess, Angela Coxon, Deborah Choquette, Karen Rex, Yihong Zhang, Daniel M. Baker, Jonathan Werner, Paul E. Hughes, Yajing Yang, Isabelle Dussault, Paula Kaplan-Lefko, Sean Caenepeel
Publikováno v:
Molecular cancer therapeutics. 15(7)
The MET receptor tyrosine kinase is involved in cell growth, survival, and invasion. Clinical studies with small molecule MET inhibitors have shown the role of biomarkers in identifying patients most likely to benefit from MET-targeted therapy. AMG 3