Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Anthony Mastracchio"'
Autor:
Junichiro Yuda, Christine Will, Darren C. Phillips, Linu Abraham, Cory Alvey, Abraham Avigdor, Wayne Buck, Lauren Besenhofer, Erwin Boghaert, Dong Cheng, Dan Cojocari, Kelly Doyle, T. Matthew Hansen, Kevin Huang, Eric F. Johnson, Andrew S. Judd, Russell A. Judge, John C. Kalvass, Aaron Kunzer, Lloyd T. Lam, Rachel Li, Ruth L. Martin, Anthony Mastracchio, Mike Mitten, Adam Petrich, Jin Wang, James E. Ward, Haichao Zhang, Xilu Wang, Johannes E. Wolff, Katherine M. Bell-McGuinn, Andrew J. Souers
Publikováno v:
Communications Medicine, Vol 3, Iss 1, Pp 1-14 (2023)
Abstract Background MCL-1 is a prosurvival B-cell lymphoma 2 family protein that plays a critical role in tumor maintenance and survival and can act as a resistance factor to multiple anticancer therapies. Herein, we describe the generation and chara
Externí odkaz:
https://doaj.org/article/a09a2953c50e4da8ad9915dfa149ffac
Autor:
Andrew J. Souers, Wei Qiu, Thomas D. Penning, Darren C. Phillips, Xiaoqin Liu, Rick F. Clark, Joel D. Leverson, Amanda M. Olson, Chunqiu Lai, Daniel H. Albert, Gui-Dong Zhu, Yunsong Tong, Peter Kovar, Kenton L. Longenecker, Anthony Mastracchio, Morey L. Smith, Bailin Shaw, Alan S. Florjancic, Stephen K. Tahir, Donald J. Osterling
Publikováno v:
ACS Med Chem Lett
[Image: see text] Cyclin-dependent kinase 9 (CDK9) is a serine/threonine kinase involved in the regulation of transcription elongation. An inhibition of CDK9 downregulates a number of short-lived proteins responsible for tumor maintenance and surviva
Autor:
Velitchka Bontcheva, Maricel Torrent, David Maag, Anthony Mastracchio, Fritz G. Buchanan, Loren M. Lasko, Debra Ferguson, Thomas D. Penning, Alexander R. Shoemaker, Kenneth D. Bromberg, Chunqiu Lai, Eric F. Johnson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1481-1486
In continuation of our previous research towards the discovery of potent, selective and drug-like Wee1 inhibitors, 2 novel series of biaryl heterocycles were designed, synthesized and evaluated. The new biaryl cores were designed to enable structure
Autor:
Chunqiu Lai, Alexander R. Shoemaker, Fritz G. Buchanan, Eric F. Johnson, David Maag, Anthony Mastracchio, Velitchka Bontcheva, Kenneth D. Bromberg, Thomas D. Penning, Debra Ferguson, Maricel Torrent, Loren M. Lasko
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:126895
Autor:
Sangita B. Patel, Scott D. Edmondson, Ann E. Weber, Reshma A. Patel, Aleksandr Petrov, Kathryn A. Lyons, Bing Zhu, Joseph K. Wu, Anthony Mastracchio, Shiyao Xu, George J. Eiermann, Ranabir Sinha Roy, Giovanna Scapin, Nancy A. Thornberry, Jason M. Cox, Huaibing He
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4097-4101
A new series of DPP-4 inhibitors derived from piperidine-fused benzimidazoles and imidazopyridines is described. Optimization of this class of DPP-4 inhibitors led to the discovery of imidazopyridine 34. The potency, selectivity, cross-species DMPK p
Autor:
Joseph K. Wu, Reshma A. Patel, Nancy A. Thornberry, Ann E. Weber, Jason M. Cox, Shiyao Xu, Bing Zhu, Barbara Leiting, Kathryn A. Lyons, Scott D. Edmondson, Ranabir Sinha Roy, Bart Harper, Huaibing He, Anthony Mastracchio
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4579-4583
Substituted 3-aminopiperidines 3 were evaluated as DPP-4 inhibitors. The inhibitors showed good DPP-4 potency with superb selectivity over other peptidases (QPP, DPP8, and DPP9). Selected DPP-4 inhibitors were further evaluated for their hERG potassi
Autor:
Joseph K. Wu, KellyAnn D. Pryor, Ann E. Weber, George J. Eiermann, Reshma A. Patel, Dooseop Kim, Jinyou Xu, Nancy A. Thornberry, Anthony Mastracchio, Scott D. Edmondson, Jennifer E. Kowalchick, Huaibing He, Barbara Leiting, Kathryn A. Lyons
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3373-3377
A series of beta-aminoamides bearing triazolopiperazines has been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. Efforts at optimization of the beta-aminoamide series, which ultimately led to th
Publikováno v:
Science. 316:582-585
The asymmetric α-addition of relatively nonpolar hydrocarbon substrates, such as allyl and aryl groups, to aldehydes and ketones remains a largely unsolved problem in organic synthesis, despite the wide potential utility of direct routes to such pro
Autor:
Reshma A. Patel, Aleksandr Petrov, Frank Marsilio, Barbara Leiting, Kathryn A. Lyons, Anthony Mastracchio, Lan Wei, Jinyou Xu, Ann E. Weber, Nancy A. Thornberry, George J. Eiermann, Joseph F. Leone, Joseph K. Wu, Scott D. Edmondson, Huaibing He, Robert J. Mathvink
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1346-1349
anti-Substituted beta-methylphenylalanine derived amides have been shown to be potent DPP-IV inhibitors exhibiting excellent selectivity over both DPP8 and DPP9. The optimized compound exhibited good pharmacokinetic profiles in three preclinical spec
Autor:
Yves Girard, Dwight Macdonald, Deborah A. Nicoll-Griffith, Michel Gallant, Nathalie Chauret, Daniel Dube, Anthony Mastracchio, Laird A. Trimble, Kevin P. Bateman, José M. Silva, Stephen Day, Helene Perrier
Publikováno v:
Journal of Mass Spectrometry. 41:771-780
L-454,560 is a potent phospodiesterase 4 (PDE4) inhibitor which was identified as a development candidate for the treatment of asthma and chronic obstructive pulmonary disease (COPD). As part of the discovery of this compound, interspecies in vitro m