Zobrazeno 1 - 10
of 82
pro vyhledávání: '"Vinod F. Patel"'
Autor:
Richard L. Kendall, Robert Radinsky, Stephanie Geuns-Meyer, Vinod F. Patel, Isabelle Dussault, Mary Stanton, Annette Bak, Laurie B. Schenkel, Karina Romero, Philip R. Olivieri, Hanh Nho Nguyen, Brian L. Hodous, Holly L. Deak, Victor J. Cee, Sandra Ross, Patricia McElroy, Patrick Eden, Beth Ziegler, Grace Chung, Tammy L. Bush, Marc Payton
Supplementary Methods, Figures 1-5 from Preclinical Evaluation of AMG 900, a Novel Potent and Highly Selective Pan-Aurora Kinase Inhibitor with Activity in Taxane-Resistant Tumor Cell Lines
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7147a5f5dbda291c8291002c611e48dd
https://doi.org/10.1158/0008-5472.22387907.v1
https://doi.org/10.1158/0008-5472.22387907.v1
Autor:
Sachin Maniar, Anlai Wang, James Pribish, Shih-Min A. Huang, Andrew Hebert, Mikhail Levit, Jinyu Liu, Claude Barberis, Luke Fire, Elina Tserlin, Paul Erdman, Vinod F. Patel, Mark Czekaj, Joseph D. Batchelor, Frank Sun
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:127625
N-substituted azaindoles were discovered as potent pan-PIM inhibitors. Lead optimization, guided by structure and focused on physico-chemical properties allowed us to solve inherent hERG and permeability liabilities, and provided compound 27, which s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ec3a40682ad7fc0c9b4c038e0e32843
https://doi.org/10.1016/j.bmcl.2020.127625
https://doi.org/10.1016/j.bmcl.2020.127625
Discovery of N-substituted 7-azaindoles as Pan-PIM kinases inhibitors - Lead optimization - Part III
Autor:
Andrew Hebert, Paul Erdman, Maniar Sachin, Anlai Wang, Alexandre Gross, Elina Tserlin, Claude Barberis, Vinod F. Patel, Jiang John Z, Mark Czekaj, Mikhail Levit, James Pribish, Frank Sun, Matthieu Barrague, Luke Fire, Shih-Min A. Huang
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(3)
N-substituted azaindoles were discovered as promising pan-PIM inhibitors. Lead optimization is described en route toward the identification of a clinical candidate. Modulation of physico-chemical properties allowed to solve inherent hERG and permeabi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c747e4800362180020faedb6eee28913
https://pubmed.ncbi.nlm.nih.gov/30553737
https://pubmed.ncbi.nlm.nih.gov/30553737
Autor:
Holly L. Deak, Richard Kendall, Chaves Mary, Robert Radinsky, Grace Chung, Annette Bak, Yang Dai, Bingfan Du, Karina R. Vaida, Min-Hwa Jasmine Lin, Hanh Nho Nguyen, Brian L. Hodous, Laurie B. Schenkel, Tammy L. Bush, Patrick Eden, Paul S. Andrews, Liyue Huang, Xuhai Be, Philip R. Olivieri, Stephanie D. Geuns-Meyer, Victor J. Cee, Kelly Hanestad, Marc Payton, Jin Tang, Vinod F. Patel, Pedro J. Beltran, Beth Ziegler
Publikováno v:
Journal of Medicinal Chemistry. 58:5189-5207
Efforts to improve upon the physical properties and metabolic stability of Aurora kinase inhibitor 14a revealed that potency against multidrug-resistant cell lines was compromised by increased polarity. Despite its high in vitro metabolic intrinsic c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::12730d02cfac93673e41d912f0563da7
https://doi.org/10.1021/acs.jmedchem.5b00183
https://doi.org/10.1021/acs.jmedchem.5b00183
Autor:
Paul H. Wen, Robert C. Wahl, Ryan White, Oleg Epstein, Stephen J. Wood, Katayoun Derakhchan, Douglas A. Whittington, Chuck E. Kreiman, Isaac E. Marx, Thomas Dineen, Dean Hickman, Kui Chen, Matthew Weiss, Joel Esmay, Vinod F. Patel, Alan C. Cheng, Robert T. Fremeau
Publikováno v:
Journal of Medicinal Chemistry. 57:9811-9831
We have previously shown that the aminooxazoline xanthene scaffold can generate potent and orally efficacious BACE1 inhibitors although certain of these compounds exhibited potential hERG liabilities. In this article, we describe 4-aza substitution o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c9b3095ff7f5efcf8cbc5e633bdfc8f
https://doi.org/10.1021/jm5012676
https://doi.org/10.1021/jm5012676
Autor:
Fangxian Sun, Laurent Schio, Carlos Garcia-Echeverria, Dietmar Hoffmann, Shih Min A Huang, Christoph Lengauer, Bailin Zhang, Vinod F. Patel, Francisco Adrian, Michel Tabart, Hong Cheng, Weidong Zhang, Anlai Wang, Qiang Gao, Zhuyan Guo, Jingxin Zhang, Claude Barberis, Stefan Gross, Josh Murtie, Jennifer Rocnik, Mikhail Levit, Dmitri Wiederschain, Marion Dorsch
Publikováno v:
Blood. 124:1777-1789
Postchemotherapy relapse presents a major unmet medical need in acute myeloid leukemia (AML), where treatment options are limited. CD25 is a leukemic stem cell marker and a conspicuous prognostic marker for overall/relapse-free survival in AML. Rare
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86fd20272c355acdbc0ebc55c54bddc6
https://doi.org/10.1182/blood-2014-01-551234
https://doi.org/10.1182/blood-2014-01-551234
Autor:
Xin Huang, Susan M. Turci, Zihao Hua, Randy Serafino, Liyue Huang, Jin Tang, Jason Brooks Human, Ryan White, Lisa Acquaviva, Jennifer Dovey, Barbara Grubinska, Oleg Epstein, Doug Saffran, Huilin Zhao, Steve Schneider, Howard Bregman, Hongbing Huang, Anne B. O’Connor, Violeta Yu, John Newcomb, Jonathan T. Goldstein, Nagasree Chakka, Matthew W. Martin, Vinod F. Patel, Craig A. Strathdee, Virginia Berry, Alexander M. Long, Cindy Wilson, Erin F. DiMauro, Hakan Gunaydin
Publikováno v:
ACS Medicinal Chemistry Letters. 3:1059-1064
Aberrant activation of the Wnt pathway is believed to drive the development and growth of some cancers. The central role of CK1γ in Wnt signal transduction makes it an attractive target for the treatment of Wnt-pathway dependent cancers. We describe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc43848aa690914df587add69f5cd2c3
https://doi.org/10.1021/ml300278f
https://doi.org/10.1021/ml300278f
Autor:
Vinod F. Patel, Thomas T. Nguyen, Lewis D. Pennington, Daniel B. Horne, Michael D. Bartberger, Holger Monenschein, Stephen Hitchcock, Wenge Zhong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3607-3611
The synthesis and SAR of a series of BACE-1 hydroxyethyl amine inhibitors containing substitutions on a spirocyclobutyl moiety is described. Selectivity against cathepsin D, a related aspartyl protease with potential off target toxicity, and improved
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ee9cf462951bcfa5784ecb95fc1ba18
https://doi.org/10.1016/j.bmcl.2012.04.060
https://doi.org/10.1016/j.bmcl.2012.04.060
Autor:
Kui Chen, Daniel La, Michael D. Bartberger, Russell Graceffa, Thomas T. Nguyen, Tisha San Miguel, E. Allen Sickmier, Ryan Brown, Vivian S. W. Li, Stephen J. Wood, Lewis D. Pennington, James Brown, Jianhua Zhang, Craig E. Masse, Holger Monenschein, Patricia Lopez, Dean Hickman, Brian K. Albrecht, May Xue, Michael Croghan, Scott Harried, Safura Babu-Khan, Yuan Cheng, Yi Luo, Martin Citron, Matthew R. Kaller, Patricia Amarante, Wenge Zhong, Paul H. Wen, Bryant Yang, Robert C. Wahl, Matthew Weiss, Chuck Kriemen, Stephen Hitchcock, Vinod F. Patel, Ted Judd, Toni Williamson
Publikováno v:
ACS Medicinal Chemistry Letters. 3:886-891
β-Secretase inhibitors are potentially disease-modifying treatments for Alzheimer's disease. Previous efforts in our laboratory have resulted in hydroxyethylamine-derived inhibitors such as 1 with low nanomolar potency against β-site amyloid precur
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1836b589b3ebfe48433f1f6f45d8355
https://doi.org/10.1021/ml3000148
https://doi.org/10.1021/ml3000148
Autor:
Yuan Cheng, Matthew R. Kaller, Steven W. Louie, Martin Citron, Lewis D. Pennington, Daniel S. La, Matthew Weiss, Stephen J. Wood, Wenge Zhong, Michael Croghan, Toni Williamson, Scott Harried, James Brown, Kui Chen, Tisha San Miguel, Ronke Imbeah-Ampiah, Holger Monenschein, Qiufen Xue, Hongbing Huang, Patricia Lopez, Claire Rattan, Thomas Dineen, Daniel B. Horne, E. Allen Sickmier, Dean Hickman, Safura Babu-Khan, Charles Kreiman, Vivian S. W. Li, Paul H. Wen, Michael D. Bartberger, Russell Graceffa, Robert C. Wahl, Thomas T. Nguyen, Bryant Yang, Ted Judd, Joel Esmay, Vinod F. Patel, Stephen Hitchcock
Publikováno v:
Journal of Medicinal Chemistry. 55:9009-9024
A series of potent hydroxyethyl amine (HEA) derived inhibitors of β-site APP cleaving enzyme (BACE1) was optimized to address suboptimal pharmacokinetics and poor CNS partitioning. This work identified a series of benzodioxolane analogues that posse
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::282a471f56ccce495f911c58f29307ea
https://doi.org/10.1021/jm300119p
https://doi.org/10.1021/jm300119p