Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Diane B. Hauze"'
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1eec816e736d1f8d7e039cc0629e060
https://doi.org/10.1016/j.bmcl.2010.02.099
https://doi.org/10.1016/j.bmcl.2010.02.099
Autor:
Weiguang Zhao, Raymond Unwalla, Frederick J. Bex, Richard J. Murrills, John A. Robinson, Nippa Alon, Usha Varadarajan, Paul J. Yaworsky, Adam M. Gilbert, Valerie E. Coleburn, Virginia Gironda, Diane B. Hauze, Matthew Kirisits, Michael C. Sharp, Paula Green, Yao-Bin Liu, Yogendra P. Kharode, Girija Krishnamurthy, Matthew Gregory Bursavich, Bheem M. Bhat, Michael Cain, Sabrina Lombardi, Jeanne J. Matteo, Sally Selim, Ho-Sun Lam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:366-370
A series of (hetero)arylpyrimidines agonists of the Wnt-beta-catenin cellular messaging system have been prepared. These compounds show activity in U2OS cells transfected with Wnt-3a, TCF-luciferase, Dkk-1 and tk-Renilla. Selected compounds show mini
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf51cfbc58bde75044a12e24b5e0086f
https://doi.org/10.1016/j.bmcl.2009.10.093
https://doi.org/10.1016/j.bmcl.2009.10.093
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::26eacb52fff02ace8eb134ea084fe282
https://doi.org/10.1021/jm9014197
https://doi.org/10.1021/jm9014197
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98e42c70637294bea6edaaf45f2b6b18
https://doi.org/10.1016/j.bmcl.2009.02.043
https://doi.org/10.1016/j.bmcl.2009.02.043
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2b2a453cf8d2bd665d3484f6156095d
https://doi.org/10.1021/jm801572m
https://doi.org/10.1021/jm801572m
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::11f80d1947f55d3348918157d5792d53
https://doi.org/10.1016/j.bmc.2008.05.024
https://doi.org/10.1016/j.bmc.2008.05.024
Autor:
Kees Kenneth L, Valerie E. Coleburn, Frederick J. Bex, Horace Fletcher, Bheem M. Bhat, Jeanne J. Matteo, Richard J. Murrills, Charles William Mann, Diane B. Hauze
Publikováno v:
Letters in Drug Design & Discovery. 2:201-204
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::aa51cedc0eef3cefda7e99a59354d7cd
https://doi.org/10.2174/1570180053765110
https://doi.org/10.2174/1570180053765110
Publikováno v:
Canadian Journal of Chemistry. 79:1632-1654
Ninhydrin is an essential tool in the analysis of amino acids, peptides, and proteins, and the preferred reagent for the detection of latent fingerprints on porous surfaces. The goal of this investigation was to prepare ninhydrin analogs with enhance
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::305f0cd99bb35948a61fe2905f72f018
https://doi.org/10.1139/v01-143
https://doi.org/10.1139/v01-143
Autor:
Rajarathnam E. Reddy, Joanna M. Szewczyk, Kelly K. Schumacher, Franklin A. Davis, Madeleine M. Joullié, Diane B. Hauze, Jianjun Jiang
Publikováno v:
Tetrahedron Letters. 40:455-458
The astin family of cyclopentapeptides contains several noncoded amino acids, including β-phenylalanine, α-aminobutyric acid and several substituted prolines. The difficult cyclization of the macrocycle and the subsequent first total synthesis of a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::dfd0e055b0b2fb2742b0233b9fbeaed5
https://doi.org/10.1016/s0040-4039(98)02423-x
https://doi.org/10.1016/s0040-4039(98)02423-x
Publikováno v:
Tetrahedron. 53:4239-4246
The synthesis of the previously reported thianinhydrin ( 12 ) was achieved from 3-methylthiophene via the corresponding 5,6-dihydrocyclopenta[ b ]thiophen-4,6-dione ( 10 ). Conversion of 10 to the tricarbonyl ( 12 ) proceeded in good yield using dime
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bb83c61212856aafef1a723e523bb435
https://doi.org/10.1016/s0040-4020(97)00151-8
https://doi.org/10.1016/s0040-4020(97)00151-8