Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Tara M. Stauffer"'
Autor:
W. Lynn Rogers, Brian F. Mcguinness, Kurt W. Saionz, Steven G. Kultgen, Vikash Srivastava, Hema Desai, Hao Yan, Tara M. Stauffer, Samiran Saha, Koc-Kan Ho, Shengting Zhang, Neelima Mannava, Yan Jiang, Anthony E. Klon, Tailong Li, Juxing Yin, Weiqing Chen, Konghua Jing, Maria L. Webb, Kanak Kanti Majumdar, Laura L. Rokosz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7414-7420
A novel series of quinolinone-based adenosine A2B receptor antagonists was identified via high throughput screening of an encoded combinatorial compound collection. Synthesis and assay of a series of analogs highlighted essential structural features
Autor:
Jocelyn Rivera, Xiaoying Xu, Haengsoon Park, Lesley Schultz, Kamil Paruch, David A. Parry, Alvarez Carmen S, Emma Lees, Thierry O. Fischmann, Doll Ronald J, Tara M. Stauffer, Laura R. Rokosz, Chad E. Knutson, Wolfgang Seghezzi, Vincent S. Madison, Alan Hruza, Michael P. Dwyer, Ray Anthony James, Derek Wiswell, Mckittrick Brian A, Greg Tucker, Frances Shanahan, Nicole Sgambellone, Kerry Keertikar, Randall R. Rossman, Timothy J. Guzi, Vidyadhar M. Paradkar, Yaolin Wang, Quiao Zhou, Paul Kirschmeier, Amin A. Nomeir, Tin-Yau Chan, Courtney Brown
Publikováno v:
ACS Medicinal Chemistry Letters. 1:204-208
Inhibition of cyclin-dependent kinases (CDKs) has emerged as an attractive strategy for the development of novel oncology therapeutics. Herein is described the utilization of an in vivo screening approach with integrated efficacy and tolerability par
Autor:
Kaiser Bernd, Aki Cynthia J, Rosemary Mayer-Ezel, Chao Jianping, R. William Hipkin, Richard W. Bond, Taveras Arthur G, Daniel Lundell, Jianhua Chao, Laura L. Rokosz, Purakkattle J. Biju, James Jakway, Viyyoor M. Girijavallabhan, Jay S. Fine, Tara M. Stauffer, James Fossetta, Wei Wang, Ge Li, Hong Bian, J. Robert Merritt, Waldemar Gonsiorek, Xuedong Fan, Baldwin John J, Michael P. Dwyer, Carol Terminelli, Younong Yu, Diane Rindgen, Lynne E. Ozgur
Publikováno v:
Journal of Medicinal Chemistry. 49:7603-7606
Structure-activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist with excellent cell-based activity. Compound 4 displayed good oral bioavailability in rat and
Autor:
Kingsley H. Nelson, Lynne E. Ozgur, Laura L. Rokosz, Adriane E. Schilling, Taveras Arthur G, Wei Wang, Kaiser Bernd, Ge Li, Chao Jianping, Tara M. Stauffer, J. Robert Merritt, Baldwin John J, Michael P. Dwyer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4107-4110
A novel series of 3,4-diaminocyclobut-3-ene-1,2-diones was prepared and found to show potent inhibitory activity of CXCR2 binding and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Microsome stability and Caco2 studies were subsequently us
Autor:
Daniel Chelsky, Eileen C. Southwick, Ge Li, Chia-Yu Huang, Tara M. Stauffer, Laura L. Rokosz, John C. Reader, Baldwin John J
Publikováno v:
Combinatorial Chemistry & High Throughput Screening. 9:545-558
The development of structure-activity relationships (SARs) relating to the function of a biological protein is often a long and protracted undertaking when using an iterative medicinal chemistry approach. High throughput screening of ECLiPS®(Encoded
Autor:
Baldwin John J, Ashit K. Ganguly, He Huang, Laura L. Rokosz, Alan B. Cooper, Doll Ronald J, Chia-Yu Huang, John C. Reader, Ge Li, Corey Strickland, Tara M. Stauffer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:507-511
Farnesyltransferase inhibitors identified from an ECLiPS® library were optimized using solution-phase synthesis. X-ray crystallography of inhibited complexes was used to identify substructures that coordinate to the active site zinc. The X-ray struc
Autor:
Nolan H. Sigal, Daniel Chelsky, Chia-Yu Huang, Ashit K. Ganguly, Laura L. Rokosz, Tara M. Stauffer, Baldwin John J, John C. Reader
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5537-5543
In order to fully explore structure-activity relationships at the 1- and 2-positions of the piperazine core of tricyclic farnesyltransferase inhibitors, an 11,718-member ECLiPS library was synthesized and screened in a farnesyltransferase scintillati
Autor:
Brian F. Mcguinness, Marc-Raleigh Brescia, Guizhen Dong, Tara M. Stauffer, Nicole White, Neelima Mannava, Catherine M. Hicks, Ian R. Henderson, Elizabeth Quadros, Yuefei Shao, Andrew G. Cole, Earl F. Kimble, Pamela G. Wines, Laura L. Rokosz
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(22)
A novel series of adenosine A2A receptor antagonists was identified by high-throughput screening of an encoded combinatorial compound collection. The initial hits were optimized for A2A binding affinity, A1 selectivity, and in vitro microsomal stabil
Autor:
Laura L. Rokosz, Ian Henderson, Lan-Ying Qin, Andrew G. Cole, Jingqi Duo, Brian F. Mcguinness, Marc-Raleigh Brescia, Tara M. Stauffer, Yuefei Shao
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(5)
A series of trisubstituted purinones was synthesized and evaluated as A(2A) receptor antagonists. The A(2A) structure-activity relationships at the three substituted positions were studied and selectivity against the A(1) receptor was investigated. O
Autor:
Lawrence W. Dillard, Wenguang Zeng, Laura L. Rokosz, Ian Henderson, Andrew G. Cole, Axel Metzger, Tara M. Stauffer
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(2)
The discovery and synthesis of a series of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A2A receptor antagonists from a small-molecule combinatorial library using a high-throughput radioligand-binding assay is described. Antagonists were furth