Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Kimberly G, Petrov"'
Autor:
Tara Renae Rheault, Kimberly N. Smitheman, Kimberly G. Petrov, Chao Han, George Adjabeng, Alex G. Waterson, Marc R. Arnone, Alastair J. King, David E. Uehling, Olivia W. Rossanese, Keith R. Hornberger, Scott Howard Dickerson, John Stellwagen, Cynthia M. Rominger, Robert A. Mook
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:4436-4440
A potent series of inhibitors against the B-RafV600E kinase have been developed that show excellent activity in cellular assays and good oral bioavailability in rats. The key structural features of the series are an arylsulfonamide headgroup, a thiaz
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15c814f8930dd9b7f17ce5a15f5e5352
https://doi.org/10.1016/j.bmcl.2011.06.021
https://doi.org/10.1016/j.bmcl.2011.06.021
Autor:
Kimberly G. Petrov, Thomas R. Caferro, Octerloney B. McDonald, David W. Rusnak, Dana E. Vanderwall, Kelly Horne Donaldson, Tara Renae Rheault, David E. Uehling, Lisa M. Shewchuk, Scott Howard Dickerson, Robert J. Mullin, Michael D. Gaul, Aaron S. Goetz, Glenn M. Spehar, Anne T. Truesdale, Edgar R. Wood
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:817-820
Two new series of potent and selective dual EGFR/ErbB-2 kinase inhibitors derived from novel thienopyrimidine cores have been identified. Isomeric thienopyrimidine cores were evaluated as isosteres for a 4-anilinoquinazoline core and several analogs
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8a62e1d36d5f76869f6a2a75d7237e2
https://doi.org/10.1016/j.bmcl.2008.12.011
https://doi.org/10.1016/j.bmcl.2008.12.011
Autor:
Alex G. Waterson, Hamilton D. Dickson, Edgar R. Wood, Michael J. Reno, Thomas R. Caferro, Douglas M. Sammond, Tara Renae Rheault, Stanley D. Chamberlain, Barry R. Keith, Holly Kathleen Emerson, Jennifer G. Badiang Alberti, Robert D. Hubbard, Robert J. Griffin, David W. Rusnak, Robert J. Mullin, Krystal J. Alligood, David E. Uehling, Stephon C. Smith, Kimberly G. Petrov, Roseanne Gerding, Scott Howard Dickerson, Kirk L. Stevens
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:21-26
A novel class of pyrrolidinyl-acetyleneic thieno[3,2-d]pyrimidines has been identified which potently inhibit the EGFR and ErbB-2 receptor tyrosine kinases. Synthetic modifications of the pyrrolidine carbamate moiety result in a range of effects on e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b009e9b77f5a50bba3b10df514e6c53b
https://doi.org/10.1016/j.bmcl.2008.11.023
https://doi.org/10.1016/j.bmcl.2008.11.023
Autor:
Kimberly G. Petrov, Ann Louise Walker, Yu Guo, Malcolm Clive Carter, David W. Rusnak, Scott Howard Dickerson, Robert A. Mook, Cassandra A. Gauthier, Edgar R. Wood, Karen Lackey, G. Stuart Cockerill, Yue-Mei Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4686-4691
Synthetic modifications on a 6-furanylquinazoline scaffold to optimize the dual ErbB-1/ErbB-2 tyrosine kinase inhibition afforded consistent SAR whereby a 4-(3-fluorobenzyloxy)-3-haloanilino provided the best enzyme potency and cellular selectivity.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb0e36c5b474465ea5bf127c87c05182
https://doi.org/10.1016/j.bmcl.2006.05.090
https://doi.org/10.1016/j.bmcl.2006.05.090
Autor:
M. Anthony Leesnitzer, Kimberly G. Petrov, Marcia L. Moss, Darryl Lynn Mcdougald, J. David Becherer, David J. Cowan, Robert W. Wiethe, Millard H. Lambert, David Lee Musso, Robert Andrews, D. Mark Bickett, Jennifer Gabriel Badiang, Michael D. Gaul, Andersen Marc W, Daniel B. Kassel, Michael H. Rabinowitz, R. Kevin Blackburn, Janet Warner, Daniel S. Kinder, Theresa D. Seaton
Publikováno v:
Combinatorial Chemistry & High Throughput Screening. 8:327-339
We report a systematic analysis of the P1' and P2' substrate specificity of TNF-alpha converting enzyme (TACE) using a peptide library and a novel analytical method, and we use the substrate specificity information to design novel reverse hydroxamate
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e9c38b38823234fe10e050a50c9a3d7a
https://doi.org/10.2174/1386207054020840
https://doi.org/10.2174/1386207054020840
Autor:
Laurie S. Kane-Carson, Kimberly N. Smitheman, Chao Han, Alex G. Waterson, Marc R. Arnone, Olivia W. Rossanese, David E. Uehling, John Stellwagen, Keith R. Hornberger, Robert A. Mook, Scott Howard Dickerson, Katherine G. Moss, Alastair J. King, Kimberly G. Petrov, Sylvie Laquerre, Ganesh S. Moorthy, George Adjabeng, Tara Renae Rheault
Hyperactive signaling of the MAP kinase pathway resulting from the constitutively active B-Raf(V600E) mutated enzyme has been observed in a number of human tumors, including melanomas. Herein we report the discovery and biological evaluation of GSK21
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87ece1513b9365faece7d7d536bde0c1
https://europepmc.org/articles/PMC4027516/
https://europepmc.org/articles/PMC4027516/
Autor:
Alex G. Waterson, Kimberly G. Petrov, Glenn M. Spehar, Robert J. Griffin, Kevin Hinkle, Keith R. Hornberger, Scott Howard Dickerson, Kirk L. Stevens, Douglas M. Sammond, Edgar R. Wood, Stephon C. Smith, Thomas R. Caferro, David W. Rusnak, Robert D. Hubbard, Hamilton D. Dickson, David E. Uehling
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(5)
Aniline ‘headgroups’ were synthesized and incorporated into an alkynyl thienopyrimidine series of EGFR and ErbB-2 inhibitors. Potent inhibition of enzyme activity and cellular proliferation was observed. In certain instances, protein binding was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3db39f0bebeac3d520429b58091c7b0f
https://pubmed.ncbi.nlm.nih.gov/19208477
https://pubmed.ncbi.nlm.nih.gov/19208477
Autor:
Sarva M. Tadepalli, Alex G. Waterson, Perry Scott Brignola, Scott Howard Dickerson, Robert J. Mullin, Thomas R. Caferro, Craig D. Wagner, Hamilton D. Dickson, Dana E. Vanderwall, Kimberly G. Petrov, John C. Ulrich, Michael D. Gaul, Lisa M. Shewchuk, Anne M. Hassell, Kelly Horne Donaldson, Edgar R. Wood, David E. Uehling, Jon D. Williams, Ronald L. Brashear, Barry R. Keith, Wendy L. White, David W. Rusnak, Byron Ellis, Robert J. Griffin, Michael J. Reno
Analysis of the x-ray crystal structure of mono-substituted acetylenic thienopyrimidine 6 complexed with the ErbB family enzyme ErbB-4 revealed a covalent bond between the terminal carbon of the acetylene moiety and the sulfhydryl group of Cys-803 at
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ee325f04de0f7f4e5e90c473b3e261b
https://europepmc.org/articles/PMC2268535/
https://europepmc.org/articles/PMC2268535/
Autor:
Millard H, Lambert, R Kevin, Blackburn, Theresa D, Seaton, Daniel B, Kassel, Daniel S, Kinder, M Anthony, Leesnitzer, D Mark, Bickett, Janet R, Warner, Marc W, Andersen, Jennifer G, Badiang, David J, Cowan, Michael D, Gaul, Kimberly G, Petrov, Michael H, Rabinowitz, Robert W, Wiethe, J David, Becherer, Darryl L, McDougald, David L, Musso, Robert C, Andrews, Marcia L, Moss
Publikováno v:
Combinatorial chemistryhigh throughput screening. 8(4)
We report a systematic analysis of the P1' and P2' substrate specificity of TNF-alpha converting enzyme (TACE) using a peptide library and a novel analytical method, and we use the substrate specificity information to design novel reverse hydroxamate
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::993edb682148101da04f2a40507a6ade
https://pubmed.ncbi.nlm.nih.gov/16101009
https://pubmed.ncbi.nlm.nih.gov/16101009
Autor:
Lee F. Kuyper, Kimberly G. Petrov, Karen Lackey, Robert N. Hunter, Edgar R. Wood, Philip A. Harris
Publikováno v:
ChemInform. 35
The discovery, synthesis, potential binding mode, and in vitro kinase profile of 3-(3-bromo-4-hydroxy-5-(2'-methoxyphenyl)-benzylidene)-5-bromo-1,3-dihydro-pyrrolo[2,3-b]pyridin-2-one, 3-[(1-methyl-1H-indol-3-yl)methylene]-1,3-dihydro-2H-pyrrolo[3,2-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4957ec60820d15446bb4553a3bb00761
https://doi.org/10.1002/chin.200423168
https://doi.org/10.1002/chin.200423168