Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Steven N. Gallicchio"'
Autor:
Scott E. Wolkenberg, Richard J. O. Barnard, Steven N. Gallicchio, Michael A. Plotkin, Douglas C. Beshore, Christine Burlein, Robert W. Myers, M. Katharine Holloway, Daniel J. Klein, Vanessa L. Rada, Christopher D. Cox, David A. Powell, Daniel Krosky, Paul J. Coleman, Gregory C. Adam, Sangita B. Patel, Wei Lemaire
Publikováno v:
ACS Medicinal Chemistry Letters
A novel series of histone deacetylase (HDAC) inhibitors lacking a zinc-binding moiety has been developed and described herein. HDAC isozyme profiling and kinetic studies indicate that these inhibitors display a selectivity preference for HDACs 1, 2,
Autor:
Harold G. Selnick, Mangay Williams, Patricia Miller, Guy Bormans, Hong Fan, Tom Reynders, Koen Van Laere, Cyrille Sur, Ruben Declercq, Rebecca L. Blanchard, Zhizhen Zeng, Eric D. Hostetler, Mona Purcell, Tjibbe de Groot, Sandra Sanabria-Bohorquez, Liza Gantert, Anne Van Hecken, Jan de Hoon, Steven N. Gallicchio, Eugene E. Marcantonio, Inge Derdelinckx, Stacey O'Malley, Stefanie A. Kane, Aniket D. Joshi, Inge De Lepeleire, Richard Hargreaves, Jacquelynn J. Cook, Ian M. Bell, Kerry Riffel, Christopher A. Salvatore, William P. Kennedy, Chi-Chung Li, Jeffrey L. Evelhoch
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 347:478-486
Calcitonin gene-related peptide (CGRP) is a potent neuropeptide whose agonist interaction with the CGRP receptor (CGRP-R) in the periphery promotes vasodilation, neurogenic inflammation and trigeminovascular sensory activation. This process is implic
Autor:
Samuel L. Graham, Joseph G. Bruno, Scott D. Mosser, Harold G. Selnick, Sandra M. Sanabria-Bohórquez, Christopher A. Salvatore, Rebecca B. White, Melody Mcwherter, Hong Fan, Mangay Williams, Jacquelynn J. Cook, Kerry Riffel, Richard Hargreaves, Ian M. Bell, Craig A. Stump, Eric L. Moore, Liza Gantert, Steven N. Gallicchio, Mona Purcell, C. Blair Zartman, Amanda L. Kemmerer, Eric D. Hostetler, Donnette D. Staas, Stefanie A. Kane
Publikováno v:
ACS Medicinal Chemistry Letters. 4:863-868
Rational modification of the potent calcitonin gene-related peptide (CGRP) receptor antagonist MK-3207 led to a series of analogues with enhanced CNS penetrance and a convenient chemical handle for introduction of a radiolabel. A number of (11)C-trac
Autor:
Samuel L. Graham, Christine Fandozzi, Eric L. Moore, Donnette D. Staas, Ian M. Bell, Nova Sain, Joseph G. Bruno, Steven N. Gallicchio, Harold G. Selnick, Christopher A. Salvatore, Mark O. Urban, Rebecca B. White, Matthew M. Zrada, Amy Calamari, C. Blair Zartman, Amanda L. Kemmerer, Joseph P. Vacca, Stefanie A. Kane, Craig A. Stump, Scott D. Mosser
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3941-3945
Rational modification of the clinically tested CGRP receptor antagonist MK-3207 (3) afforded an analogue with increased unbound fraction in rat plasma and enhanced aqueous solubility, 2-[(8R)-8-(3,5-difluorophenyl)-8-methyl-10-oxo-6,9-diazaspiro[4.5]
Autor:
Christopher P. Regan, Zhizhen Zeng, David L. Williams, Harold G. Selnick, Rebecca B. White, John F. Fay, Amy Calamari, Cyrille Sur, Stacey O'Malley, Stefanie A. Kane, Samuel Graham, Joseph P. Vacca, Andrew Danziger, Christopher A. Salvatore, Eric L. Moore, Patricia Miller, Maria S. Michener, Nicole T. Pudvah, Steven N. Gallicchio, Jacquelynn J. Cook, Ian M. Bell, Joseph J. Lynch, Yui S. Tang, Chi-Chung Li
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 333:152-160
Calcitonin gene-related peptide (CGRP) has long been hypothesized to play a key role in migraine pathophysiology, and the advent of small-molecule antagonists has clearly demonstrated a clinical link between blocking the CGRP receptor and migraine ef
Autor:
Xu-Fang Zhang, Samuel L. Graham, Theresa M. Williams, Craig A. Stump, Victor K. Johnston, Scott D. Mosser, Joseph G. Bruno, C. Blair Zartman, Steven N. Gallicchio, Joseph P. Vacca, Eric L. Moore, Christopher A. Salvatore, John F. Fay, Rodney A. Bednar, Amy G. Quigley, Cory R. Theberge, Ian M. Bell, Stefanie A. Kane
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:214-217
Rational modification of a previously identified spirohydantoin lead structure has identified a series of potent spiroazaoxindole CGRP receptor antagonists. The azaoxindole was found to be a general replacement for the hydantoin that consistently imp
Autor:
Diem N. Nguyen, Samuel L. Graham, Theresa M. Williams, Scott D. Mosser, Ian M. Bell, Bang-Lin Wan, Kimberly Della Penna, Priya Kunapuli, Stefanie A. Kane, Craig A. Stump, Ruth Z. Rutledge, John F. Fay, Ken S. Koblan, Joseph P. Vacca, C. Blair Zartman, Steven N. Gallicchio, Amy G. Quigley, Christopher A. Salvatore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:2595-2598
High-throughput screening of the Merck sample collection identified benzodiazepinone tetralin-spirohydantoin 1 as a CGRP receptor antagonist with micromolar activity. Comparing the structure of 1 with those of earlier peptide-based antagonists such a
Autor:
Jin Hua, J. Christopher Culberson, David C. Heimbrook, B. Wesley Trotter, Steven M. Stirdivant, Annette S. Kim, Dawn L. Hall, Christopher J. Dinsmore, Maria Kornienko, C. Blair Zartman, Steven N. Gallicchio, Theresa M. Williams, Ian M. Bell, Samuel L. Graham, Lloyd Waxman, John C. Reid, Nathan R. Kett, Paul L. Darke, Ahern Janet, Sanjeev Munshi, Lawrence C. Kuo, Robert A. Drakas, Amy G. Quigley
Publikováno v:
Biochemistry. 44:9430-9440
The type 1 insulin-like growth factor receptor (IGF-1R) is often overexpressed on tumor cells and is believed to play an important role in anchorage-independent proliferation. Additionally, cell culture studies have indicated that IGF-1R confers incr
Autor:
Kelly Hamilton, Michael J. Bogusky, Robert B. Lobell, Lorena S. Beese, Joel R. Huff, Samuel L. Graham, Marc Abrams, Jackson B. Gibbs, Christine Fernandes, Ronald G. Robinson, J. Christopher Culberson, Carl F. Homnick, Eileen S. Walsh, Joseph J. Lynch, David C. Heimbrook, Michelle Ellis-Hutchings, Douglas C. Beshore, Hans E. Huber, Kenneth S. Koblan, Jeffrey S. Taylor, George D. Hartman, Hema Bhimnathwala, Kelem Kassahun, Nancy E. Kohl, Theresa M. Williams, Carolyn A. Buser, A. David Rodrigues, Joseph P. Davide, C. Blair Zartman, Steven N. Gallicchio, Ian M. Bell
Publikováno v:
Journal of Medicinal Chemistry. 45:2388-2409
A series of macrocyclic 3-aminopyrrolidinone farnesyltransferase inhibitors (FTIs) has been synthesized. Compared with previously described linear 3-aminopyrrolidinone FTIs such as compound 1, macrocycles such as 49 combined improved pharmacokinetic
Autor:
Theresa M. Williams, A. David Rodrigues, Douglas C. Beshore, Carolyn A. Buser, Joseph P. Davide, Michelle Ellis-Hutchings, Steven N. Gallicchio, J. Christopher Culberson, Samuel L. Graham, George D. Hartman, Marc Abrams, David C. Heimbrook, and Eileen S. Walsh, Carl F. Homnick, Kenneth S. Koblan, Joel R. Huff, Robert B. Lobell, Joseph J. Lynch, Christine Fernandes, Patricia A. Miller, Jackson B. Gibbs, Charles A. Omer, Kelem Kassahun, Nancy E. Kohl, Ian M. Bell
Publikováno v:
Journal of Medicinal Chemistry. 44:2933-2949
The synthesis, structure-activity relationships, and biological properties of a novel series of imidazole-containing inhibitors of farnesyltransferase are described. Starting from a 3-aminopyrrolidinone core, a systematic series of modifications prov