Zobrazeno 1 - 10
of 54
pro vyhledávání: '"Edward Pack"'
Autor:
Adam Flegg, Tina Morwick, Ho Yin Lo, Todd Bosanac, Weimin Liu, Valentina Berger, Steven Kerr, Stéphane De Lombaert, Paige Erin Mahaney, Ralph Binetti, John Broadwater, Spencer Napier, Alessandra Bartolozzi, Lifen Wu, Hidenori Takahashi, Asitha Abeywardane, Heather Tye, Tazmeen Fadra-Khan, John D. Huber, Adrian Kotey, Ming-Hong Hao, Dines Jonathon Alan, Anil Kumar Padyana, Alan Olague, Michael Garrigou, David S. Thomson, J. Matthew Hutzler, Pui Leng Loke, Renee Zindell, Edward Pack, Zhidong Chen, Rebecca Crux, Thomas Simpson, Rajvee Dave, Doris Riether
Publikováno v:
Journal of Medicinal Chemistry. 58:1669-1690
The synthesis, structure–activity relationship (SAR), and evolution of a novel series of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitors are described. The use of structure-guided drug design techniques provided compounds
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ec30afc1732226a8a2acaaba6be03b4
https://doi.org/10.1021/jm501185j
https://doi.org/10.1021/jm501185j
Autor:
Christian Harcken, Richard M. Nelson, Daniel Kuzmich, Tazmeen Fadra-Khan, Edward Pack, Jörg Bentzien, Donald Souza, Darren Disalvo, Alison Kukulka, David S. Thomson, Raj Betageri, Gerald Nabozny
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6640-6644
A class of α-methyltryptamine sulfonamide glucocorticoid receptor (GR) modulators was optimized for agonist activity. The design of ligands was aided by molecular modeling, and key function-regulating pharmacophoric points were identified that are c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::373ffd38700c5c8cbd1180416e3625b3
https://doi.org/10.1016/j.bmcl.2013.10.052
https://doi.org/10.1016/j.bmcl.2013.10.052
Autor:
Eugene R. Hickey, Anthony S. Prokopowicz, George E. Lee, Carol Ann Homon, Scott Jakes, Wang Mao, Jun Li, Charlene Peng, Bennett T. Farmer, Scott F. Leonard, Mohammed A. Kashem, Kevin Chungeng Qian, Charles L. Cywin, Lian Wang, Ronald Magboo, Morgan Welzel, John P. Wolak, Edward Pack, Tina Morwick
Publikováno v:
Journal of Medicinal Chemistry. 52:1814-1827
A series of inhibitors of Pim-2 kinase identified by high-throughput screening is described. Details of the hit validation and lead generation process and structure-activity relationship (SAR) studies are presented. Disclosure of an unconventional bi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40bdff6788836da6a99ef9f5bd96cab0
https://doi.org/10.1021/jm801242y
https://doi.org/10.1021/jm801242y
Autor:
Ming-Hong Hao, Andre White, Edward Pack, Zhaoming Xiong, Daniel R. Goldberg, Donghong Amy Gao, Brian Werneburg, Donna Skow, Derek Cogan, Thomas Trieselmann, Neil Moss, Chris Pargellis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1994-1999
Chemistry has been developed to specifically functionalize two structurally similar classes of indole-based MK2 inhibitors at positions prompted by a combination of X-ray crystallographic and computer assisted drug design. A gain in molecular potency
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8589aebcbef0a2ad460d66cb80340749
https://doi.org/10.1016/j.bmcl.2008.01.119
https://doi.org/10.1016/j.bmcl.2008.01.119
Autor:
Louise K. Modis, Yong Wang, Stephanie M. Ng, Sulagna Sanyal, Brian Nicholas Cook, Lemieux Rene M, Melissa Hill-Drzewi, Younggi Choi, Wei Xu, Kristina Gueneva-Boucheva, Diva Sze-Ming Chan, Lori Patnaude, Edward Pack, Eugene R. Hickey, Michael B. Fisher, Can Mao, Horan Joshua Courtney, Lynne Canne Bannen, Steve Fogal, Morrison B. Mac, Shawn Anderson
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(20)
The discovery of a new series of selective S1P1 agonists is described. This series of piperazinyl-oxadiazole derivatives was rapidly optimized starting from high-throughput screening hit 1 to afford potent and selective lead compound 10d. Further SAR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9c1d02c0a100a8aa396d81b0aed901e7
https://pubmed.ncbi.nlm.nih.gov/25241927
https://pubmed.ncbi.nlm.nih.gov/25241927
Autor:
Donald Souza, Mark Panzenbeck, Jörg Bentzien, Tazmeen Fadra-Khan, Carol A. Torcellini, Roger M. Dinallo, Christian Harcken, Hossein Razavi, Alison Kukulka, Gerald Nabozny, Ljiljana Zuvela-Jelaska, David S. Thomson, Richard M. Nelson, Josephine Pelletier, Edward Pack, Doris Riether, John R. Proudfoot
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(8)
Synthesis and structure-activity relationship (SAR) of a series of alkyl and cycloalkyl containing non-steroidal dissociated glucocorticoid receptor (GR) agonists is reported. This series of compounds was identified as part of an effort to replace th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b9a3d38ce00c671a4e81b5135c46af55
https://pubmed.ncbi.nlm.nih.gov/24656565
https://pubmed.ncbi.nlm.nih.gov/24656565
Autor:
Angela Berry, Edward Pack, Gerald Nabozny, Alison Kukulka, Kirrane Thomas M, Daniel Kuzmich, Raj Betageri, Jörg Bentzien, Richard M. Nelson, Carol A. Torcellini, Bachir Latli, Christian Harcken, Mark Panzenbeck, Tazmeen N. Fadra, Roger M. Dinallo, Ljiljana Zuvela-Jelaska, Gilmore Thomas A, Don Souza, Heewon Lee, Josephine Pelletier, Younes Bekkali, Dieter Wiedenmayer, John R. Regan, Susan E. Goldrick, David S. Thomson
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(22)
We report a SAR of non-steroidal glucocorticoid mimetics that utilize indoles as A-ring mimetics. Detailed SAR is discussed with a focus on improving PR and MR selectivity, GR agonism, and in vitro dissociation profile. SAR analysis led to compound (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a0894392651eead7a62f90ba3b953fd
https://pubmed.ncbi.nlm.nih.gov/21963986
https://pubmed.ncbi.nlm.nih.gov/21963986
Autor:
Josephine Pelletier, Jörg Bentzien, Doris Riether, Richard M. Nelson, David S. Thomson, Tazmeen N. Fadra, Roger M. Dinallo, Daniel Kuzmich, Gerald Nabozny, Donald Souza, Alison Kukulka, Ljiljana Zuvela-Jelaska, Gilmore Thomas A, Mark Panzenbeck, Edward Pack, Christian Harcken, Carol A. Torcellini, Hossein Razavi
Publikováno v:
Journal of medicinal chemistry. 53(18)
Syntheses and structure−activity relationships (SAR) of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain azaindole moieties as A-ring mimetics and display various degrees of in vitro dissociation between gen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ffc2413c5f4218a8c1f3ea1d2613039
https://pubmed.ncbi.nlm.nih.gov/20735001
https://pubmed.ncbi.nlm.nih.gov/20735001
Autor:
Kevin Qian, Lian Wang, Charles L. Cywin, Bennett T. Farmer, Eugene Hickey, Carol Homon, Scott Jakes, Mohammed A. Kashem, George Lee, Scott Leonard, Jun Li, Ronald Magboo, Wang Mao, Edward Pack, Charlene Peng, Anthony Prokopowicz, Morgan Welzel, John Wolak, Tina Morwick
Publikováno v:
Journal of Medicinal Chemistry; Apr2009, Vol. 52 Issue 7, p1814-1827, 14p
Autor:
Robert S. Magnant, Anthony G. Oettinger, Carol L. Weinhaus, Clayton L. Hallmark, Fred B. Wood, Rolla Edward Pack, William A. Lucas
Publikováno v:
Communication Booknotes. 10:215-216
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6a535412a4526d832fce05871eb2086e
https://doi.org/10.1080/10948007909489163
https://doi.org/10.1080/10948007909489163