Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Thomas R. Caferro"'
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:
Esther Martinborough, Donald S. Karanewsky, Francisco J. López, Robert I. Higuchi, Min Wu, William Y. Chang, Marquis L. Cummings, Lin Zhi, Thomas Lau, Yun Oliver Long, Thomas R. Caferro, Keith B. Marschke
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2967-2971
Modification on a lead series of [1,4]oxazino[3,2-g]quinolin-7-ones at the 2-position led to selective androgen receptor modulators with improved in vivo activity. The most potent analog (-)-33a exhibited full maintenance of levator ani muscle at 3mg
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::552333f5b43ce9586e4d20f15f4bb123
https://doi.org/10.1016/j.bmcl.2008.03.062
https://doi.org/10.1016/j.bmcl.2008.03.062
Autor:
Jyun-Hung Chen, Thomas R. Caferro, Charlotte Pooley Deckhut, Lin Zhi, Christopher M. Tegley, Keith B. Marschke, Anthony W. Thompson, James P. Edwards, E. Adam Kallel, Marquis L. Cummings, Francisco J. López, William T. Schrader, Robert I. Higuchi, Mark E. Adams, Donald S. Karanewsky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5442-5446
A series of androgen receptor modulators based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones was synthesized and evaluated in an androgen receptor transcriptional activation assay. The most potent analogues from the series exhibited single-digit nanomolar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb24be52ff66235cfadff901d5d77fd6
https://doi.org/10.1016/j.bmcl.2007.07.034
https://doi.org/10.1016/j.bmcl.2007.07.034
Autor:
James P. Edwards, James W. Kong, Kristen L. Arienti, Keith B. Marschke, Thomas R. Caferro, Robert I. Higuchi, Luc J. Farmer, Robert L. Davis, Todd K. Jones, Josef D. Ringgenberg, Lawrence G. Hamann
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:1335-1340
A series of human androgen receptor (hAR) agonists based on 4-alkyl-; 4,4-dialkyl-; and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinoline was synthesized and evaluated in competitive receptor binding assays and an androgen receptor cotransfec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6263b53da9f5d576664b6452d5408f4
https://doi.org/10.1016/s0960-894x(99)00186-9
https://doi.org/10.1016/s0960-894x(99)00186-9
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:
Neelakhanda S. Mani, Dale E. Mais, Francisco J. López, Kristen L. Arienti, Lin Zhi, Yun Oliver Long, William T. Schrader, Todd K. Jones, James P. Edwards, and Andrés Negro-Vilar, Thomas R. Caferro, Keith B. Marschke, Robert I. Higuchi
Publikováno v:
Journal of medicinal chemistry. 50(10)
Recent interest in orally available androgens has fueled the search for new androgens for use in hormone replacement therapy and as anabolic agents. In pursuit of this, we have discovered a series of novel androgen receptor modulators derived from 7H
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0419b3636b9e469778f1a83a511d76c2
https://pubmed.ncbi.nlm.nih.gov/17439112
https://pubmed.ncbi.nlm.nih.gov/17439112
Autor:
Mark E. Goldman, Robert I. Higuchi, Lawrence G. Hamann, Lin Zhi, Pooley Charlotte L F, James P. Edwards, Todd K. Jones, David T. Winn, Thomas R. Caferro, Keith B. Marschke
Publikováno v:
Bioorganicmedicinal chemistry letters. 9(7)
A series of 2 H -pyrano[3,2- g ]quinolin-2-ones was prepared and tested for the ability to modulate the transcriptional activity of the human androgen receptor (hAR). The parent compound, 4-(trifluoromethyl)-2 H -pyrano[3,2- g ]quinolin-2-one display
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d9eddff2fb854ed60d8e8c8e8e376c3c
https://pubmed.ncbi.nlm.nih.gov/10230628
https://pubmed.ncbi.nlm.nih.gov/10230628
Autor:
Robert I. Higuchi, Kristen L. Arienti, Francisco J. López, Neelakhanda S. Mani, Dale E. Mais, Thomas R. Caferro, Yun Oliver Long, Todd K. Jones, James P. Edwards, Lin Zhi, William T. Schrader, Andrés Negro-Vilar, Keith B. Marschke
Publikováno v:
Journal of Medicinal Chemistry; May2007, Vol. 50 Issue 10, p2486-2496, 11p