Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Barri Wautlet"'
Autor:
Jennifer Brown, Karen E. Parrish, Andrew J. Tebben, Jonathan Lippy, Kamalavenkatesh Palanisamy, Todd Kinsella, Chetan Padmakar Darne, Vinay K. Holenarsipur, Anwar Murtaza, Muthalagu Vetrichelvan, Chunhong Yan, Karen Augustine-Rauch, Max Ruzanov, Mark Fereshteh, Upender Velaparthi, Gopal Dhar, Gregory D. Vite, Peiying Liu, Steven Sheriff, Jayakumar Sankara Warrier, Aravind Anandam, Marina Gelman, Arvind Mathur, Barri Wautlet, Robert M. Borzilleri, Hasibur Rahaman, Zheng Yang, Anuradha Gupta, Arun Kumar Gupta, Rajinder Singh, Joseph Fargnoli, Jesse Swanson
Publikováno v:
ACS Med Chem Lett
[Image: see text] Novel imidazole-based TGFβR1 inhibitors were identified and optimized for potency, selectivity, and pharmacokinetic and physicochemical characteristics. Herein, we report the discovery, optimization, and evaluation of a potent, sel
Autor:
Barri Wautlet, Lalgudi S. Harikrishnan, Jonathan Lippy, Andrew J. Tebben, Amol G. Dikundwar, P.N. Arunachalam, Raju Mannoori, Max Ruzanov, Yi Fan, Gopikishan Tonukunuru, Vishweshwaraiah Baligar, Mark Fereshteh, Balaji Seshadri, Jayakumar Warrier, Sudhakara R. Madduri, Joseph Fargnoli, Robert M. Borzilleri, Ching-Ping Ho, Brian E. Fink, Steven Sheriff, Hasibur Rahaman
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:1026-1034
The TGFβ-TGFβR signaling pathway has been reported to play a protective role in the later stages of tumorigenesis via increasing immunosuppressive Treg cells and facilitating the epithelial to mesenchymal transition (EMT). Therefore, inhibition of
Autor:
Yufen Zhao, Barri Wautlet, Jonathan Lippy, Anne Rose, Andrew J. Tebben, Gregory D. Vite, Max Ruzanov, Joseph Fargnoli, Liping Zhang, Yong Zhang, Zheng Yang, Karen E. Parrish, Robert M. Borzilleri, Yi Fan, Jesse Swanson, Ching-Ping Ho, Karen Augustine-Rauch, Andrew F. Donnell, Brian E. Fink, Steven Sheriff, Mark Fereshteh
[Image: see text] The multifunctional cytokine TGFβ plays a central role in regulating antitumor immunity. It has been postulated that inhibition of TGFβ signaling in concert with checkpoint blockade will provide improved and durable immune respons
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dca61cd13f527f4d17df3df6c932c4f3
https://europepmc.org/articles/PMC6231184/
https://europepmc.org/articles/PMC6231184/
Autor:
David K. Williams, Kristen A. Kellar, Louis J. Lombardo, Veeraswamy Manne, Joseph Fargnoli, John S. Tokarski, Xiao-Tao Chen, Robert Jeyaseelan, Yongmi An, Barri Wautlet, Robert M. Borzilleri, George L. Trainor, Robert F. Kaltenbach, Benjamin J. Henley, Christine M. Tarby, John S. Sack, Zhen-Wei Cai, Johnni Gullo-Brown
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2998-3002
Biarylamine-based inhibitors of Met kinase have been identified. Lead compounds demonstrate nanomolar potency in Met kinase biochemical assays and significant activity in the Met-driven GTL-16 human gastric carcinoma cell line. X-ray crystallography
Autor:
Rajeev S. Bhide, Daniel W. Kukral, Harold Malone, Barri Wautlet, John T. Hunt, Anne Lewin, Joel C. Barrish, Bala Krishnan, Steven Mortillo, Joseph Fargnoli, Zhen-Wei Cai, Louis J. Lombardo, Benjamin J. Henley, Susan Galbraith, Robert Jeyaseelan
Publikováno v:
Molecular Cancer Therapeutics. 9:369-378
Tumor angiogenesis is a complex and tightly regulated network mediated by various proangiogenic factors. The fibroblast growth factor (FGF) and vascular endothelial growth factor (VEGF) family of growth factors, and associated tyrosine kinase recepto
Autor:
Robert J. Schmidt, Benjamin J. Henley, Celia D’Arienzo, Jonathan Lippy, John S. Sack, Yueping Zhang, Yongmi An, John T. Hunt, Amrita Kamath, John S. Tokarski, Barri Wautlet, Veeraswamy Manne, Dianlin Xie, Punit Marathe, Donna D. Wei, Louis J. Lombardo, Kyoung S. Kim, Robert Jeyaseelan, David K. Williams, Joseph Fargnoli, Liping Zhang, Yaquan Zhang, Johnni Gullo-Brown, Zhen-Wei Cai, George L. Trainor, Robert M. Borzilleri
Publikováno v:
Journal of Medicinal Chemistry. 51:5330-5341
Conformationally constrained 2-pyridone analogue 2 is a potent Met kinase inhibitor with an IC50 value of 1.8 nM. Further SAR of the 2-pyridone based inhibitors of Met kinase led to potent 4-pyridone and pyridine N-oxide inhibitors such as 3 and 4. T
Autor:
Ligang Qian, Carl Thibeault, Amrita Kamath, Barri Wautlet, Alain Martel, George L. Trainor, Punit Marathe, Celia D’Arienzo, Benjamin J. Henley, Steven Mortillo, Donna D. Wei, Robert Jeyaseelan, Ravindra W. Tejwani, John T. Hunt, Louis J. Lombardo, Rejean Ruel, Yueping Zhang, Zhen-Wei Cai, Joseph Fargnoli, Arvind Mathur, Alexandre L'Heureux, Joel C. Barrish, Rajeev S. Bhide, George M. Derbin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2985-2989
We report herein a series of substituted N-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amines as inhibitors of vascular endothelial growth factor receptor-2 tyrosine kinase. Through structure–activity relationship studies, biochem
Autor:
Celia D’Arienzo, Daniel W. Kukral, Stephanie Barbosa, Steve Mortillo, John T. Hunt, Lawrence Wu, Punit Marathe, George M. Derbin, Joseph Fargnoli, Yong-Zheng Zhang, Robert M. Borzilleri, Joel C. Barrish, Zhongping Shi, Jeffrey A. Robl, Robert Jeyaseelan, Rajeev S. Bhide, Ligang Qian, Donna D. Wei, Junying Fan, Amrita Kamath, Xiaoping Zheng, Zhen-Wei Cai, Louis J. Lombardo, Barri Wautlet
Publikováno v:
Journal of Medicinal Chemistry. 51:1976-1980
A series of amino acid ester prodrugs of the dual VEGFR-2/FGFR-1 kinase inhibitor 1 (BMS-540215) was prepared in an effort to improve the aqueous solubility and oral bioavailability of the parent compound. These prodrugs were evaluated for their abil
Autor:
Joseph Fargnoli, Daniel W. Kukral, Steve Mortillo, Viral Vyas, John S. Tokarski, John T. Hunt, Robert M. Borzilleri, Rajeev S. Bhide, Robert Jeyaseelan, Louis J. Lombardo, Amrita Kamath, Xiaoping Zheng, Ligang Qian, Barri Wautlet, Zhen-Wei Cai, Joel C. Barrish, Aberra Fura, Christopher D. Ellis
Publikováno v:
Journal of Medicinal Chemistry. 48:3991-4008
A series of substituted 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines was identified as potent and selective inhibitors of the tyrosine kinase activity of the growth factor receptors VEGFR-2 (Flk-1, KDR) and FGFR-1. T
Autor:
Raj N. Misra, William G. Humphreys, K R Webster, John S. Sack, Y. F. Kelly, Janet G. Mulheron, Kimball Sd, Ligang Qian, Sam T. Chao, Kyoung S. Kim, Leslie Leith, John T. Hunt, Barri Wautlet, John S. Tokarski
Publikováno v:
Journal of Medicinal Chemistry. 43:4126-4134
Flavopiridol analogues, thio- and oxoflavopiridols which contain a sulfur (16) or oxygen (18) atom linker between a chromone ring and the hydrophobic side chain, are selective cyclin-dependent kinase 1 (CDK1) inhibitors with an IC(50) of 110 and 130