Zobrazeno 1 - 10
of 77
pro vyhledávání: '"Mark W. Holladay"'
Autor:
Mark W. Holladay, Shripad S. Bhagwat, Michael Williams, Bruce D. Dorsey, Raffaella Faraoni, Julius L. Apuy, Mark A. Ator, Darren E. Insko, Mehran Yazdanian, Dana Gitnick, Mangeng Cheng, Ronald R. Nepomuceno, Kathryn Hunter, Merryl D. Cramer, Hugh Zhao, Michael F. Gardner, Pawel Dobrzanski, Ruwanthi N. Gunawardane, Susan Jones-Bolin, Martin W. Rowbottom, Robert C. Armstrong, Bruce Ruggeri, Joyce James
PDF file - 74K, CEP-32496 Supplemental Data.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e595ddea4dcb7e0d0c551afc2da871ae
https://doi.org/10.1158/1535-7163.22498993.v1
https://doi.org/10.1158/1535-7163.22498993.v1
Autor:
Sheena Quiambao, Ruwanthi N. Gunawardane, Dana Gitnick, Mindy I. Davis, Shawn R. Eichelberger, Mike A. Breider, Robert C. Armstrong, Gang Liu, Lan Tran, Michael F. Gardner, Michael J. Hadd, Julia M. Ford Pulido, Julius L. Apuy, Sunny Abraham, Barbara Belli, Joyce James, Helen Hua, Mark W. Holladay, Troy D. Vickers, Shimin Xu, Daniel K. Treiber
Publikováno v:
Journal of Medicinal Chemistry. 55:3250-3260
Serine/threonine protein kinases Aurora A, B, and C play essential roles in cell mitosis and cytokinesis. Currently a number of Aurora kinase inhibitors with different isoform selectivities are being evaluated in the clinic. Herein we report the disc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::abd16747c2507b55eee6e7c2341a5e8b
https://doi.org/10.1021/jm201702g
https://doi.org/10.1021/jm201702g
Autor:
Michael J. Hadd, Helen Hua, Gang Liu, Dana Gitnick, Troy D. Vickers, Lan Tran, Janice A. Sindac, Joyce James, Zdravko V. Milanov, Robert C. Armstrong, Daniel K. Treiber, Mark W. Holladay, Julia M. Ford Pulido, Merryl D. Cramer, Barbara Belli, Shripad Bhagwat, Alan Dao, Sunny Abraham
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5296-5300
The synthesis and SAR for a novel series of pyrrolotriazines as pan-Aurora kinase inhibitors are described. Optimization of the cyclopropane carboxamide terminus of lead compound 1 resulted in analogs with high cellular activity and improved rat PK p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::97442310ba09dc49a99ab34d58bc3932
https://doi.org/10.1016/j.bmcl.2011.07.027
https://doi.org/10.1016/j.bmcl.2011.07.027
Publikováno v:
Biochemical Pharmacology. 74:1092-1101
Neuronal nicotinic acetylcholine receptors (nAChRs) have been a target for drug discovery efforts, primarily for CNS indications, for the past two decades. While nicotine and related natural products have been used for smoking cessation in various fo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::556c1e072670efcf6daede25faea19a1
https://doi.org/10.1016/j.bcp.2007.06.033
https://doi.org/10.1016/j.bcp.2007.06.033
Autor:
Barbara Belli, Alan Dao, Robert C. Armstrong, Michael F. Gardner, Darren E. Insko, Sunny Abraham, Ron R. Nepomuceno, Gang Liu, Mark W. Holladay, Dana Gitnick, Daniel Brigham, Patrick P. Zarrinkar, Shimin Xu, Xing Liu, Allison M. Rooks, Ron Christopher
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(17)
Based on a putative binding mode of quizartinib (AC220, 1), a potent FMS-like tyrosine kinase 3 (FLT3) inhibitor in Phase III clinical development, we have designed de novo a simpler aminopyridine-based hinge binding motif. Further optimization focus
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::109fecdca0b1b404a04804a76856a998
https://pubmed.ncbi.nlm.nih.gov/26208887
https://pubmed.ncbi.nlm.nih.gov/26208887
Autor:
Rodger F. Henry, Steven A. Buckner, Michael E. Brune, Tracy L. Carr, Sweta P. Katwala, Masaki Nakane, Thomas R. Miller, Arthur A. Hancock, Jorge D. Brioni, Anthony V. Daza, Michael Meyer, John C Cain, William A. Carroll, Robert J. Altenbach, Albert Khilevich, Lynne M. Ireland, Fan Yang, Mark W. Holladay, Meena V. Patel, Rohde Jeffrey J, William H. Bunnelle, Chae H Kang, Timothy A. Esbenshade, Donna M. Gauvin, Teodozyj Kolasa, James P. Sullivan, Karin R. Tietje, Jane Kuk, Pramila Bhatia, Alyssa B. O'Neill, Searle Xenia B, Ivan Milicic, Erol K. Bayburt
Publikováno v:
Journal of Medicinal Chemistry. 47:3220-3235
Structure-activity studies were performed on the alpha(1A)-adrenoceptor (AR) selective agonist N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide (4). Compounds were evaluated for binding activity at the alpha(1A), alpha(1b)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5013ae295bf243228c84c7a005bf8f58
https://doi.org/10.1021/jm030551a
https://doi.org/10.1021/jm030551a
Autor:
Irene Drizin, Jorge D. Brioni, Michael E. Kort, Hao Bai, Michael C. Fitzgerald, Robert J. Gregg, Linda L. King, Robert J. Altenbach, William A. Carroll, Lin Yi, Michael J. Coghlan, Rodger F. Henry, Rui Tang, Anthony V. Daza, Henry Zhang, Murali Gopalakrishnan, Michael E. Brune, Steven A. Buckner, Kristi L. Whiteaker, Thomas A. Fey, Sean C. Turner, Christopher Cassidy, Mark W. Holladay, Yiyuan Chen, Philip R. Kym, Ivan Milicic, James P. Sullivan
Publikováno v:
Journal of Medicinal Chemistry. 47:3163-3179
Structure−activity relationships were investigated on a novel series of sulfonyldihydropyridine-containing KATP openers. Ring sizes, absolute stereochemistry, and aromatic substitution were evaluated for KATP activity in guinea pig bladder cells us
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::48701963d5335233e58180eb726e63f5
https://doi.org/10.1021/jm030356w
https://doi.org/10.1021/jm030356w
Autor:
Kristi L. Whiteaker, Steven A. Buckner, James P. Sullivan, Sujatha M. Gopalakrishnan, Zhang Henry Q, Mark W. Holladay, Murali Gopalakrishnan, William A. Carroll, Lin Yi, Irene Drizin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1481-1484
A novel series of tricyclic dihydropyrimidines was synthesized and evaluated for activity as K(ATP) channel openers. The functional activity of several compounds, for example 6A (EC(50)=30nM) and its enantiomers exceeded cromakalim.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8712ef75a8bebbfb8d1ced23a0d10e3
https://doi.org/10.1016/s0960-894x(02)00207-x
https://doi.org/10.1016/s0960-894x(02)00207-x
Autor:
Richard B. Silverman, Mark W. Holladay
Chapter 6 addresses the mechanism of action of agents that target nucleic acids (DNA or RNA) to achieve their biological effects. First, the key structural properties of nucleic acids that account for their interactions with small molecules are discu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::83be31eaeceeef9ddfcb9c8dddc5fad9
https://doi.org/10.1016/b978-0-12-382030-3.00006-4
https://doi.org/10.1016/b978-0-12-382030-3.00006-4