Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Timothy Alan Grese"'
Autor:
Alan David Palkowitz, Marta Pineiro-Nunez, Abdelaziz Mahoui, Timothy Alan Grese, Maria Alvim-Gaston, Ian A. Watson
Publikováno v:
Current Topics in Medicinal Chemistry. 14:294-303
The continued development of computational and synthetic methods has enabled the enumeration or preparation of a nearly endless universe of chemical structures. Nevertheless, the ability of this chemical universe to deliver small molecules that can b
Autor:
David Andrew Neel, Karen M. Zimmerman, Matthew L. Brown, Prabhakar Kondaji Jadhav, Robert Anthony Doti, Defauw Jean Marie, Stephon C. Smith, Peter Ambrose Lander, Sally Ann Kelley, Todd Fields, Timothy Alan Grese, Mitchell I. Steinberg
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2553-2557
Syntheses and SAR studies of 3,3-bisaryloxindole analogues provided potent mineralocorticoid receptor (MR) antagonists that were selective over other steroid nuclear hormone receptors.
Autor:
Patrick I. Eacho, Thomas P. Burris, Laura F. Michael, Patricia S. Foxworthy, Jeff McCowan, Timothy Alan Grese, William W. Chin, Kuo-Long Yu, Chahrzad Montrose, Jeffrey S. Thomas, Guoqing Cao, Anton Daniel Kiefer, Denis McCann, Kelli S. Bramlett
Publikováno v:
Journal of Biological Chemistry. 278:2403-2410
Fenofibrate is clinically successful in treating hypertriglyceridemia and mixed hyperlipidemia presumably through peroxisome proliferator-activated receptor alpha (PPARalpha)-dependent induction of genes that control fatty acid beta-oxidation. Lipid
Autor:
Jeffrey Alan Dodge, Timothy Alan Grese, Henry Uhlman Bryant, Masahiko Sato, Charles H. Turner
Publikováno v:
Journal of Medicinal Chemistry. 42:1-24
Autor:
Matthew D. Belvo, Michael Gregory Bell, Douglas Linn Gernert, V. Scott Sharp, Joseph H. Kennedy, Hannah Yu, Peter Stanley Borromeo, Timothy Alan Grese, Sally Ann Kelley, Gregory A. Stephenson, Mitchell I. Steinberg, Prabhakar Kondaji Jadhav, Jeffrey D. Williams, Karen M. Zimmerman, Rachel N. Richey, Stanley P. Kolis, Peter Ambrose Lander
Publikováno v:
Journal of Medicinal Chemistry. 50:6443-6445
A novel, potent series of indole analogs were recently developed as MR antagonists, culminating in 14. This compound represents the first MR antagonist in this class of molecules, exhibiting picomolar binding affinity and in vivo blood pressure lower
Autor:
Andrew L. Glasebrook, Lorri L. Short, Harlan W. Cole, Ellen R. Rowley, James P. Sluka, David Lynn Phillips, Venugopalan M, Fuson Tr, Magee David Edward, Lewis D. Pennington, Na N. Yang, Masahiko Sato, Adrian, Timothy Alan Grese, Henry Uhlman Bryant, Pamela K. Shetler
Publikováno v:
Journal of Medicinal Chemistry. 41:1272-1283
The 2-arylbenzothiophene raloxifene, 1, is a selective estrogen receptor modulator (SERM) which is currently under clinical evaluation for the prevention and treatment of postmenopausal osteoporosis. In vivo structure-activity relationships and molec
Autor:
George Joseph Cullinan, Mark A. Winter, Na N. Yang, Alan David Palkowitz, Charles David Jones, John David Termine, James P. Sluka, Andrew L. Glasebrook, Timothy Alan Grese, Jeffrey Alan Dodge, Henry Uhlman Bryant, Masahiko Sato, Ken Matsumoto
Publikováno v:
Proceedings of the National Academy of Sciences. 94:14105-14110
Interaction of the estrogen receptor/ligand complex with a DNA estrogen response element is known to regulate gene transcription. In turn, specific conformations of the receptor-ligand complex have been postulated to influence unique subsets of estro
Autor:
Martin Michael John, Lewis D. Pennington, Andrew L. Glasebrook, Timothy Alan Grese, Ken Matsumoto, D. Lynn Phillips, Lorri L. Short
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:887-892
Methodology has been employed that permits the differentiation of the phenols of raloxifene. Transition metal mediated transformations of raloxifene triflates have subsequently provided a number of analogs that were evaluated further in two in vitro
Autor:
Andrews L. Glasebrook, Pam K. Shetler, D. Lynn Phillips, Lorri L. Short, Magee David Edward, Harlan W. Cole, Henry Uhlman Bryant, Timothy Alan Grese
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:2683-2686
The naturally occurring estrogen mimetic coumestrol has been shown to stimulate proliferation of MCF-7 mammary tumor cells and to cause uterotrophic effects in ovariectomized (OVX) rats. Attachment of a basic amine-containing sidechain to C-6 of coum
Autor:
Magee David Edward, Masahiko Sato, James P. Sluka, Timothy Alan Grese, Henry Uhlman Bryant, John Kim, Ellen R. Rowley, Harlan W. Cole
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:903-908
Several 2,3-diarylbenzopyrans have been evaluated in an ovariectomized rat model and found to exhibit tissue selective estrogen agonist activity on bone and serum lipid parameters. A structural model that accounts for the pharmacological similarity o