Zobrazeno 1 - 10
of 36
pro vyhledávání: '"Joseph T. Lundquist"'
Autor:
Charles William Mann, Lloyd M. Garrick, Matthew D. Vera, Linda Shanno, Jeffrey C. Pelletier, John F. Rogers, Diane B. Hauze, Jay E. Wrobel, Daniel M. Green, Irene Feingold, Murty Chengalvala, John F. Mehlmann, Joseph T. Lundquist, Joshua E. Cottom
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2512-2515
Antagonism of the gonadotropin releasing hormone (GnRH) receptor has resulted in positive clinical results in reproductive tissue disorders such as endometriosis and prostate cancer. Following the recent discovery of orally active GnRH antagonists ba
Autor:
Diane B. Hauze, Michael C. Sharp, Bheem M. Bhat, Paula Green, Colleen Milligan, Daniel M. Green, Jennifer Pirrello, Peter V.N. Bodine, Ronald L. Magolda, Adam M. Gilbert, Matthew D. Vera, Yogendra P. Kharode, Valerie E. Coleburn, Luciana De Araujo Felix, Mattew G. Bursavich, Nipa Alon, Jeanne J. Matteo, Jay Wrobel, Frederick J. Bex, Jeffrey C. Pelletier, Susan Lockhead, Joseph T. Lundquist, Richard J. Murrills, Ray Unwalla, Paul J. Yaworsky, Sally Selim, John F. Mehlmann, Ho-Sun Lam
Publikováno v:
Journal of Medicinal Chemistry. 52:6962-6965
A high-throughput screening campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a 2-aminopyrimidine template that targeted the Wnt beta-catenin cellular messaging system. Hit-t
Autor:
Mark J. Evans, Paige Erin Mahaney, Jay E. Wrobel, Matthew L. Crawley, Ray Unwalla, Kim Callain Younghee, John F. Mehlmann, Joseph T. Lundquist, Douglas C. Harnish
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5289-5292
Pyrrole[2,3-d]azepines have been identified as potent agonists of the farnesoid X receptor (FXR). Based on the planar X-ray crystal structure of WAY-362450 1 in the ligand binding domain and molecular modeling studies, non-planar reduced compounds we
Autor:
Lloyd M. Garrick, John F. Mehlmann, Diane B. Hauze, Joshua E. Cottom, Daniel M. Green, Jeffrey C. Pelletier, Murty Chengalvala, Irene Feingold, Joseph T. Lundquist, John F. Rogers, Charles William Mann, Linda Shanno, Jay E. Wrobel, Christine Huselton, Wenling Kao, Kees Kenneth L
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1986-1990
A previous report described the serum LH suppression pharmacology of the 2-phenyl-4-piperazinyl-benzimidazole N-ethyluracil GnRH receptor antagonist 1 following oral administration in rats. A series of small heterocycles were appended to the 2-(4-ter
Autor:
William R. Adams, Irene Feingold, John F. Mehlmann, Cesario O Tio, Joshua E. Cottom, Jay E. Wrobel, Jeffrey C. Pelletier, Daniel M. Green, John F. Rogers, James W. Jetter, Murty Chengalvala, Joseph T. Lundquist, Charles William Mann, Linda Shanno, Ronald L. Magolda, Diane B. Hauze, Gregory S. Kopf, Christine Huselton
Publikováno v:
Journal of Medicinal Chemistry. 52:2148-2152
A potent, highly insoluble, GnRH antagonist with a 2-phenyl-4-piperazinylbenzimidazole template and a quinoxaline-2,3-dione pharmacophore was modified to maintain GnRH antagonist activity and improve in vitro pharmaceutical properties. Structural cha
Autor:
Murty V. Chengalvala, Linda Shanno, Charles William Mann, Josh Cottom, Diane B. Hauze, Jay E. Wrobel, Irene Feingold, Jeffrey C. Pelletier, Gregory S. Kopf, Daniel M. Green, John A. Rogers, Wenling Kao, Christine Huselton, John F. Mehlmann, Joseph T. Lundquist, Lloyd M. Garrick, James W. Jetter
Publikováno v:
Bioorganic & Medicinal Chemistry. 16:6617-6640
Antagonism of the gonadotropin releasing hormone (GnRH) receptor has shown positive clinical results in numerous reproductive tissue disorders such as endometriosis, prostate cancer and others. Traditional therapy has been limited to peptide agonists
Publikováno v:
The Journal of Peptide Research. 59:55-61
A series of neurotensin (NT)(8-13) analogs featuring substitution of the Arg8 and/or Arg9 residues with non-natural cationic amino acids was synthesized and evaluated for binding to the human NT receptor-1 (hNTR-1). The modifications were designed to
Autor:
Joseph T. Lundquist, Thomas A. Dix
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2579-2582
Cyclic analogues of neurotensin (NT) C-terminal fragments NT(8-13) and NT(9-13) were produced via intramolecular nucleophilic substitution of the Tyr(11) phenoxide anion on a 6-bromohexanoyl side chain substituted at position 8 or 9 and tested for NT
Publikováno v:
Tetrahedron: Asymmetry. 9:2739-2743
A series of protected ω-mercapto amino acids with side-chain lengths ranging from 3–5 methylene units has been synthesized via nucleophilic substitution of ω-bromo-α-azido acids by 4-methoxy-α-toluenethiol followed by reduction of the azido fun
Autor:
Joseph T. Lundquist, Thomas A. Dix
Publikováno v:
Tetrahedron Letters. 39:775-778
A series of ω-bromo-2(S)-azido acids with side-chain lengths ranging from 3–5 methylene units has been synthesized. These intermediates enable the facile synthesis of chiral non-natural amino acids containing virtually any nucleophile capable of s