Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Robert I. Higuchi"'
Autor:
Yuan Chen, Matthew R. Durk, Lionel Rouge, Peter A. S. Smith, Man-Wah Tan, John S. Wai, Jacob Schwarz, Tucker C. Roberts, Jing Kang, Donghong Yan, Hany S. Girgis, Summer Park, John G. Quinn, Min Xu, Prasuna Paraselli, Christopher E. Heise, Jeremy Murray, Wilson Phung, Yongsheng Chen, James J. Crawford, Robert I. Higuchi, Zhiyong Yu, Michael F. T. Koehler, Elizabeth Skippington, Hua Zhang
Publikováno v:
Nature. 561:189-194
Multidrug-resistant bacteria are spreading at alarming rates, and despite extensive efforts no new class of antibiotic with activity against Gram-negative bacteria has been approved in over fifty years. Natural products and their derivatives have a k
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::51ec234ca5fb6e9853f7b3be3f183058
https://doi.org/10.1038/s41586-018-0483-6
https://doi.org/10.1038/s41586-018-0483-6
Autor:
Angela Vassar, Jeffrey N. Miner, Andrew R. Hudson, Mark E. Adams, Steven L. Roach, Dale E. Mais, Zhi Lin, Peter M. Syka, Keith B. Marschke, Robert I. Higuchi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1697-1700
A series of tetrahydroquinoline derivatives were synthesized and profiled for their ability to act as glucocorticoid receptor selective modulators. Structure-activity relationships of the tetrahydroquinoline B-ring lead to the discovery of orally ava
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e0d5bfdc37e57a78325b09cb3103b36
https://doi.org/10.1016/j.bmcl.2011.01.093
https://doi.org/10.1016/j.bmcl.2011.01.093
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:
Jeffrey N. Miner, Deepa Rungta, Lino J. Valdez, Yongkai Li, Andrew Hudson, William W. Lamph, Jean Yen, Dean P. Phillips, and Andrés Negro-Vilar, Lin Zhi, Angie Vassar, Catalina Cuervo, Reid P. Bissonnette, Keith B. Marschke, E. Adam Kallel, Mark E. Adams, Catherine J. Gharbaoui, Robert I. Higuchi, Dale E. Mais, Steven L. Roach
Publikováno v:
Journal of Medicinal Chemistry. 50:4699-4709
Structure-activity relationship studies centered around 3'-substituted (Z)-5-(2'-(thienylmethylidene))1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-chromeno[3,4-f]quinolines are described. A series of highly potent and efficacious selective glu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05412f680737616f8ba796c02fb26df7
https://doi.org/10.1021/jm070370z
https://doi.org/10.1021/jm070370z
Autor:
Robert I. Higuchi, Todd K. Jones, Arjan van Oeveren, Barbara Pio, Lin Zhi, Min Wu, Andres Negro-Vilar, Christopher M. Tegley, Keith B. Marschke
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1523-1526
A series of alkylamino-2-quinolinone compounds (3) was discovered as androgen receptor modulators based on an early linear tricyclic quinoline pharmacophore (1). The series demonstrated selective high binding affinity to androgen receptor and potent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0049481585dbb5d66ebe1f96b6191278
https://doi.org/10.1016/j.bmcl.2007.01.007
https://doi.org/10.1016/j.bmcl.2007.01.007
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:
Robert I. Higuchi, James P. Edwards, Min Wu, Jyun-Hung Chen, Chen Penghui, Neelakandha S. Mani
Publikováno v:
Tetrahedron Letters. 49:1903-1905
An efficient synthesis of the androgen receptor modulator ( R )- 4a having an 8 H -[1,4]oxazino[2,3- f ]quinolin-8-one skeleton is described. Synthesis of this ring system, not readily accessible by classical Knorr cyclization methodology, was accomp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::cd16845268058a51e4b986d27bd85680
https://doi.org/10.1016/j.tetlet.2008.01.114
https://doi.org/10.1016/j.tetlet.2008.01.114
Autor:
Robert I. Higuchi, Barry M. Trost and
Publikováno v:
Journal of the American Chemical Society. 118:10094-10105
The factors that influence the stereocontrol of trimethylenemethane (TMM) cycloadditions are examined in the context of a synthesis of a perhydroazulene. The diastereofacial selectivity with respect to the acceptor is established in an intramolecular
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3f7f428dc73544a31a683842a922a376
https://doi.org/10.1021/ja961561m
https://doi.org/10.1021/ja961561m
Autor:
Steven L. Roach, Zhi Lin, Robert I. Higuchi, Dale E. Mais, Angie Vassar, Keith B. Marschke, Andrew R. Hudson, Mark E. Adams, Lino J. Valdez, Peter M. Syka, Deepa Rungta
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(6)
Continuing studies based on dihydroquinoline glucocorticoid receptor agonists lead to the discovery of a series of C4-oxime analogs. Representative compounds exhibited potent transrepression activity with minimal transactivation of phosphoenolpyruvat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8745ea569901b5f442caef5469dcc805
https://pubmed.ncbi.nlm.nih.gov/21324689
https://pubmed.ncbi.nlm.nih.gov/21324689