Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Jeffrey G. Varnes"'
Autor:
Jeffrey W. Johannes, Fiona Pachl, Amber Balazs, Tieguang Yao, C. Larner, Lisa McWilliams, Marianne Schimpl, Scott W. Martin, Kevin J. Embrey, Tom D. Heightman, Paul Hemsley, Jonathan P. Orme, Derek Barratt, Giuditta Illuzzi, Andrew Madin, Paolo Di Fruscia, Avipsa Ghosh, Martin J. Packer, Scott D. Edmondson, Elisabetta Leo, Xiaolan Zheng, Matthew D. Chuba, Xiaohui Pei, Mark J. O'Connor, Verity Talbot, Ke Zhang, Stephen Fawell, Elizabeth Underwood, Anna Staniszewska, Lina Liu, Lin Xue, Sonja J. Gill, Anders Gunnarsson, Andrew Pike, Susan E. Critchlow, Jeffrey G. Varnes, Andrew X. Zhang, Sébastien L. Degorce, J. Lane, Sudhir M. Hande, Hongyao She, Sabina Cosulich, Michal Bista
Publikováno v:
Journal of Medicinal Chemistry. 64:14498-14512
Poly-ADP-ribose-polymerase (PARP) inhibitors have achieved regulatory approval in oncology for homologous recombination repair deficient tumors including BRCA mutation. However, some have failed in combination with first-line chemotherapies, usually
Autor:
Shenghua Wen, Srividya B. Balachander, Francis D. Gibbons, Michael Zinda, William McCoull, Nancy Su, Barry R. Davies, Stephen E. Kurtz, Terry MacIntyre, Edward J. Hennessy, Martin Wild, Paula Lewis, Ricky W. Johnstone, Jamal Carlos Saeh, Kathleen A. Burke, Omid Tavana, Andrea Newbold, Elizabeth A. Coker, Alwin Schuller, Justin Cidado, Diebold R Bruce, Tristan J. Lubinski, Steven Criscione, J. Paul Secrist, Kate Byth, Gareth P. Gregory, Deborah Lawson, Ammar Adam, Shannon K. McWeeney, Stephen Fawell, Thomas Gero, Jeffrey G. Varnes, Eric Gangl, Patricia Jaaks, Jeffrey W. Tyner, Mathew J. Garnett, Areya Tabatabai, Stephanos Ioannidis
Publikováno v:
Clinical Cancer Research. 26:6535-6549
Purpose: Targeting Bcl-2 family members upregulated in multiple cancers has emerged as an important area of cancer therapeutics. While venetoclax, a Bcl-2–selective inhibitor, has had success in the clinic, another family member, Bcl-xL, has also e
Autor:
Tieguang Yao, Liangwei Wu, Craig S. Donald, Douglas Ferguson, Lei Wang, Andrew Pike, Jianyan Wang, Justin Cidado, Dedong Wu, Kurt Gordon Pike, Kumar Thakur, Chungang Gu, Calum Cook, James Horstick, Tyler Grebe, Theresa Proia, Darren Stead, Alexander Hird, Michelle Lamb, Wenlin Shao, Nichole O'Connell, Yun Jiang, Sudhir M. Hande, Bin Yang, Janet Hawkins, Barlaam Bernard Christophe, Neil Sumner, Melissa Vasbinder, Andrew D. Ferguson, Jane E. Moore, Jeffrey G. Varnes, Bryan Roberts, Maryann San Martin, Lisa Drew, Ujjal Sarkar, Allan Dishington, Chris De Savi, Robert Casella, Steve C. Glossop, Jane L. Holmes, Thomas M. McGuire
Publikováno v:
Journal of Medicinal Chemistry. 63:15564-15590
A CDK9 inhibitor having short target engagement would enable a reduction of Mcl-1 activity, resulting in apoptosis in cancer cells dependent on Mcl-1 for survival. We report the optimization of a series of amidopyridines (from compound 2), focusing o
Autor:
Michael J. Tucker, Thomas A. Moss, James S. Scott, Barlaam Bernard Christophe, Paul R. J. Davey, Ryan Greenwood, Stephen Stokes, Gary Fairley, Radoslaw Polanski, Holia Hatoum-Mokdad, David Longmire, Eric Gangl, Bin Yang, Andrew Lister, Jeffrey G. Varnes
Publikováno v:
ACS Med Chem Lett
[Image: see text] Herein we describe our efforts using a late stage functionalization together with more traditional synthetic approaches to generate fluorinated analogues of the clinical candidate AZD9833. The effects of the addition of fluorine on
Autor:
Lei Wang, Allan Dishington, Jane E. Moore, Kurt Gordon Pike, Wenlin Shao, Andrew Lister, Anil Patel, Lorraine A. Hassall, Sudhir M. Hande, Jane L. Holmes, Douglas Ferguson, Thomas M. McGuire, Jeffrey G. Varnes, Lin Xue, Chungang Gu, Tieguang Yao, Barlaam Bernard Christophe, Lisa Drew, Janet Hawkins, Liangwei Wu, Chris De Savi, Melissa Vasbinder, Andrew D. Ferguson, Darren Stead, Ujjal Sarkar, Michelle Lamb, Nichole O'Connell, Bin Yang, Alexander Hird
Publikováno v:
Journal of medicinal chemistry. 64(20)
Optimization of a series of azabenzimidazoles identified from screening hit 2 and the information gained from a co-crystal structure of the azabenzimidazole-based lead 6 bound to CDK9 led to the discovery of azaindoles as highly potent and selective
Autor:
Teresa Klinowska, J. Willem M. Nissink, Hoan K. Huynh, Jason Breed, Christopher J. Morrow, Paul R. J. Davey, Thomas A. Moss, Jeffrey G. Varnes, Rodrigo J. Carbajo, James S. Scott, Bin Yang, Radoslaw Polanski, Ryan Greenwood
Publikováno v:
ACS Med Chem Lett
[Image: see text] Herein we report the use of metathesis to construct a novel tetracyclic core in a series of estrogen receptor degraders. This improved the chemical stability, as assessed using an NMR-MS based assay, and gave a molecule with excelle
Autor:
Haixia Wang, Stefan Kavanagh, Radoslaw Polanski, Eric Gangl, Michael J. Tucker, Jason Breed, Thomas Anthony Hunt, Paul R. J. Davey, Mandy Lawson, Darren Stead, Oona Delpuech, Ye Wu, J. Willem M. Nissink, Barlaam Bernard Christophe, Dedong Wu, Sudhir M. Hande, Amber Balazs, Dermot F. McGinnity, Wenzhan Yang, Thomas A. Moss, Bin Yang, Sladjana Gagrica, Kumar Thakur, Stacey Marden, Tyler Grebe, Daniel Hillebrand O'donovan, Teresa Klinowska, Samantha Jayne Hughes, Kara Herlihy, David I Fisher, Stephen Stokes, Holia Hatoum-Mokdad, Tony Johnson, James S. Scott, Elisabetta Chiarparin, Bo Peng, Sophie L. M. Janbon, Scott Throner, Ryan Greenwood, David Matthew Wilson, Andrew Lister, Stephen Fawell, Hoan Huynh, Jeffrey G. Varnes, Christopher J. Morrow, Rodrigo J. Carbajo
Publikováno v:
Journal of medicinal chemistry. 63(23)
Herein we report the optimization of a series of tricyclic indazoles as selective estrogen receptor degraders (SERD) and antagonists for the treatment of ER+ breast cancer. Structure based design together with systematic investigation of each region
Autor:
Gaochao Tian, William Frietze, Michael W. Wood, Christopher R. Holmquist, Todd Andrew Brugel, William E. Palmer, Hui Xiong, Deidre E. Wilkins, Glen Ernst, William Potts, Lindsay Hinkley, Janet Marie Forst, Xia Wang, Jeffrey S. Albert, Cristobal Alhambra, Gary Steelman, Jeffrey G. Varnes, Gerald Jonak, Don Andisik, Bruce Dembofsky, Chris Allan Veale
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1043-1049
A series of isoquinuclidine benzamides as glycine uptake inhibitors for the treatment of schizophrenia are described. Potency, lipophilicity, and intrinsic human microsomal clearance were parameters for optimization. Potency correlated with the natur
Autor:
Tyler Grebe, Ye Wu, Sudhir M. Hande, Mark Cornebise, Lakshmaiah Gingipalli, Jeffrey G. Varnes, Scott Throner, Edward J. Hennessy, Valerie Hoesch, Hoan Huynh
Publikováno v:
Tetrahedron Letters. 58:1709-1713
The preparation of a range of 1,5-disubstituted tetrazoles has been achieved through palladium-catalyzed Suzuki coupling. Using appropriately substituted 5-p-toluenesulfonyltetrazoles as substrates (obtained by cycloaddition of a substituted azide wi
Autor:
Anil Patel, Rebecca E. Meadows, Kurt Gordon Pike, Jane E. Moore, Turner Paul, Darren Stead, Barlaam Bernard Christophe, Andrew Stark, Jemma Clark, Janet Hawkins, Bin Yang, Bryan Roberts, Craig S. Donald, Gemma Davison, Esther Moore, Chris De Savi, Tyler Grebe, Calum Cook, Melissa Vasbinder, Simon C. C. Lucas, Andrew Lister, Jeffrey G. Varnes, Kumar Thakur, Sudhir M. Hande, Jane L. Holmes, Thomas M. McGuire, Alexander Hird, Allan Dishington
Publikováno v:
Tetrahedron Letters. 57:4718-4722
As part of a medicinal chemistry program, we adapted known synthetic methods for the late-stage diversification of 2,4-substituted 7-azaindoles. The strengths and weaknesses of these strategies are discussed. In the course of this work, three optimiz