Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Michael J, Ardolino"'
Autor:
David A. Candito, Vladimir Simov, Anmol Gulati, Solomon Kattar, Ryan W. Chau, Blair T. Lapointe, Joey L. Methot, Duane E. DeMong, Thomas H. Graham, Ravi Kurukulasuriya, Mitchell H. Keylor, Ling Tong, Gregori J. Morriello, John J. Acton, Barbara Pio, Weiguo Liu, Jack D. Scott, Michael J. Ardolino, Theodore A. Martinot, Matthew L. Maddess, Xin Yan, Hakan Gunaydin, Rachel L. Palte, Spencer E. McMinn, Lisa Nogle, Hongshi Yu, Ellen C. Minnihan, Charles A. Lesburg, Ping Liu, Jing Su, Laxminarayan G. Hegde, Lily Y. Moy, Janice D. Woodhouse, Robert Faltus, Tina Xiong, Paul Ciaccio, Jennifer A. Piesvaux, Karin M. Otte, Matthew E. Kennedy, David Jonathan Bennett, Erin F. DiMauro, Matthew J. Fell, Santhosh Neelamkavil, Harold B. Wood, Peter H. Fuller, J. Michael Ellis
Publikováno v:
Journal of Medicinal Chemistry. 65:16801-16817
Autor:
David A, Candito, Vladimir, Simov, Anmol, Gulati, Solomon, Kattar, Ryan W, Chau, Blair T, Lapointe, Joey L, Methot, Duane E, DeMong, Thomas H, Graham, Ravi, Kurukulasuriya, Mitchell H, Keylor, Ling, Tong, Gregori J, Morriello, John J, Acton, Barbara, Pio, Weiguo, Liu, Jack D, Scott, Michael J, Ardolino, Theodore A, Martinot, Matthew L, Maddess, Xin, Yan, Hakan, Gunaydin, Rachel L, Palte, Spencer E, McMinn, Lisa, Nogle, Hongshi, Yu, Ellen C, Minnihan, Charles A, Lesburg, Ping, Liu, Jing, Su, Laxminarayan G, Hegde, Lily Y, Moy, Janice D, Woodhouse, Robert, Faltus, Tina, Xiong, Paul, Ciaccio, Jennifer A, Piesvaux, Karin M, Otte, Matthew E, Kennedy, David Jonathan, Bennett, Erin F, DiMauro, Matthew J, Fell, Santhosh, Neelamkavil, Harold B, Wood, Peter H, Fuller, J Michael, Ellis
Publikováno v:
Journal of medicinal chemistry. 65(24)
Inhibition of leucine-rich repeat kinase 2 (LRRK2) kinase activity represents a genetically supported, chemically tractable, and potentially disease-modifying mechanism to treat Parkinson's disease. Herein, we describe the optimization of a novel ser
Autor:
Derun Li, William P. Kaplan, Cayetana Zarate, Matthew L. Maddess, Kaitlyn Marie Logan, Hongming Li, Peter Fuller, Zhiguo Jake Song, Meng Chen, Michael J. Ardolino, Jing Su, Luis E. Torres, Gregori J. Morriello
Publikováno v:
Organic Process Research & Development. 25:642-647
The application of bicyclo[1.1.1]pentanes (BCPs) as phenyl bioisosteres has garnered significant attention, as these structural motifs can improve the physiochemical profiles of drug candidates. De...
Autor:
Mitchell H. Keylor, Anmol Gulati, Solomon D. Kattar, Rebecca E. Johnson, Ryan W. Chau, Kaila A. Margrey, Michael J. Ardolino, Cayetana Zarate, Kelsey E. Poremba, Vladimir Simov, Gregori J. Morriello, John J. Acton, Barbara Pio, Xin Yan, Rachel L. Palte, Spencer E. McMinn, Lisa Nogle, Charles A. Lesburg, Donovon Adpressa, Shishi Lin, Santhosh Neelamkavil, Ping Liu, Jing Su, Laxminarayan G. Hegde, Janice D. Woodhouse, Robert Faltus, Tina Xiong, Paul J. Ciaccio, Jennifer Piesvaux, Karin M. Otte, Harold B. Wood, Matthew E. Kennedy, David Jonathan Bennett, Erin F. DiMauro, Matthew J. Fell, Peter H. Fuller
Publikováno v:
Journal of medicinal chemistry. 65(1)
The leucine-rich repeat kinase 2 (LRRK2) protein has been genetically and functionally linked to Parkinson's disease (PD), a disabling and progressive neurodegenerative disorder whose current therapies are limited in scope and efficacy. In this repor
Autor:
Theodore A. Martinot, Xavier Fradera, Meredeth A. McGowan, Wensheng Yu, Heidi Ferguson, Purakattle J Biju, H. Zhou, Nicolas Solban, Qinglin Pu, Yongxin Han, Xiao Wang, Kun Liu, Ravi Kurukulasuriya, Yu-hong Lam, Abdelghani Achab, Karin M. Otte, Michael J. Ardolino, Amy C. Doty, Charles A. Lesburg, J. Richard Miller, Yongqi Deng, Mangeng Cheng, Hongjun Zhang, Ian Knemeyer, Nunzio Sciammetta, David Jonathan Bennett
Publikováno v:
ACS Med Chem Lett
[Image: see text] Checkpoint inhibitors have demonstrated unprecedented efficacy and are evolving to become standard of care for certain types of cancers. However, low overall response rates often hamper the broad utility and potential of these break
Autor:
Josep Saurí, Michael J. Ardolino, Zhiguo J. Song, Lu Chen, Daniel J. Muzzio, Lushi Tan, Thomas Vickery, Jingjun Yin, Ji Qi, Chaomin Li, Yu-hong Lam, Ralph Zhao, Theodore A. Martinot, Matthew L. Maddess
Publikováno v:
Organic Process Research & Development. 23:1178-1190
The development of a stereospecific synthesis of a IDO1-selective inhibitor is described. The synthetic strategy toward enabling early discovery efforts along with additional findings pertaining to...
Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors
Autor:
Blair T. Lapointe, Jack D. Scott, Xin Cindy Yan, Haiqun Tang, Janice D Woodhouse, Kaleen Konrad Childers, Robert Faltus, Erin F. DiMauro, Solomon Kattar, Charles S. Yeung, Ravi Kurukulasuriya, Vladimir Simov, Hakan Gunaydin, Anmol Gulati, Joey L. Methot, Rachel L. Palte, Ellen C. Minnihan, Greg Morriello, J. Michael Ellis, Harold B. Wood, Santhosh Neelamkavil, Karin M. Otte, Michael J. Ardolino, Barbara Pio, Ping Liu, Laxminarayan G Hegde, Matthew J. Fell, Vanessa L. Rada, Peter Fuller, Paul J Ciaccio
Publikováno v:
RSC Med Chem
The discovery of potent, kinome selective, brain penetrant LRRK2 inhibitors is the focus of extensive research seeking new, disease-modifying treatments for Parkinson's disease (PD). Herein, we describe the discovery and evolution of a picolinamide-d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c8d45ea7dd7adda70471298a4476afa
https://europepmc.org/articles/PMC8292993/
https://europepmc.org/articles/PMC8292993/
Autor:
Michael J. Ardolino, Brandon A. Wright
Publikováno v:
The Journal of Organic Chemistry. 84:4670-4679
α-Arylations of cyclopropyl and related nitriles provide access to important synthetic intermediates and pharmacophores for biologically active molecules. However, robust methods for coupling of sterically encumbered partners have remained elusive.
Publikováno v:
Advanced Synthesis & Catalysis. 355:3413-3419
Kinetic resolution during the catalytic allyl-propargyl cross-coupling with chiral starting materials can be accomplished with a chiral Palladium catalyst. These reactions offer ready access to enantiomerically enriched enyne products from simple rea
Autor:
Michael J. Ardolino, James P. Morken
Publikováno v:
Journal of the American Chemical Society. 134:8770-8773
The palladium-catalyzed cross-coupling of chiral propargyl acetates and allyl boronates delivers chiral 1,5-enynes with excellent levels of chirality transfer and can be applied across a broad range of substrates.