Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Tazmeen N. Fadra"'
Autor:
Michel J. Emmanuel, Jonathan T. Reeves, Christian Harcken, Raj Betageri, Richard M. Nelson, Jörg Bentzien, Gerald Nabozny, Alison Kukulka, Ljiljana Zuvela-Jelaska, Tazmeen N. Fadra, Roger M. Dinallo, Donald Souza, Doris Riether, Mark Stephen Ralph, David S. Thomson, Angela Berry, Daniel Kuzmich, Pingrong Liu
Publikováno v:
Journal of Medicinal Chemistry. 57:1583-1598
Synthesis and structure-activity relationship (SAR) of a series of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain "diazaindole" moieties and display different transcriptional regulatory profiles in vitro and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1e6fcde7b564a7f668cbef134972ed1
https://doi.org/10.1021/jm4019178
https://doi.org/10.1021/jm4019178
Autor:
Derek Cogan, Ming-Hong Hao, Neil Moss, Christopher Pargellis, Tazmeen N. Fadra, E.C. Breinlinger, Rachel R. Kroe, Daniel R. Goldberg, Alan David Swinamer, Ronald A. Aungst, Kevin Chungeng Qian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3251-3255
A computer-aided drug design strategy leads to the identification of a new class of p38 inhibitors based on the 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) scaffold. The tolyl triazole amides provided a potent platform amenable to optimization. Furthe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::215b6ccc05dd94d4c4e84795ae2f9242
https://doi.org/10.1016/j.bmcl.2008.04.043
https://doi.org/10.1016/j.bmcl.2008.04.043
Autor:
Tazmeen N. Fadra, Kirrane Thomas M, Carol A. Torcellini, Christopher Pargellis, Neil Moss, Jeffrey B. Madwed, Rachel R. Kroe, John R. Regan, Raj Betageri, Pier F. Cirillo, Eugene R. Hickey, Kevin Chungeng Qian, Richard M. Nelson, Steffen Breitfelder, Alan David Swinamer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4242-4247
Discovery of the pyrazole-naphthyl urea class of p38 MAP kinase inhibitors typified by the clinical candidate BIRB 796 has encouraged further exploration of this particular scaffold. Modification to the part of the inhibitor that occupies the adenine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d3cd9ec3c838e1f95bbedb8d62f3936
https://doi.org/10.1016/j.bmcl.2007.05.042
https://doi.org/10.1016/j.bmcl.2007.05.042
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:
Michele Tsang, Christopher Pargellis, Alan David Swinamer, Rajiv Sharma, Kirrane Thomas M, Kevin Chungeng Qian, Pier F. Cirillo, Carol A. Torcellini, Matthew R. Netherton, Zhaoming Xiong, Neil Moss, Rachel R. Kroe, Eugene R. Hickey, Usha R. Patel, Steffen Breitfelder, Jeffrey B. Madwed, Faith Corbo Gaenzler, Daniel R. Goldberg, Sanxing Sun, Moriak Monica Helen, Victor Marc Kamhi, Hidenori Takahashi, Tazmeen N. Fadra, Gilmore Thomas A, Raj Betageri
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(9)
An effort aimed at exploring structural diversity in the N-pyrazole-N′-naphthylurea class of p38 kinase inhibitors led to the synthesis and characterization of N-phenyl-N′-naphthylureas. Examples of these compounds displayed excellent inhibition
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59cd06394b4e5ed174828058be6d3172
https://pubmed.ncbi.nlm.nih.gov/19356929
https://pubmed.ncbi.nlm.nih.gov/19356929
Autor:
Nathan K. Yee, Jeffrey B. Madwed, Clare Zimmitti, Angela Berry, Tazmeen N. Fadra, Jinhua J. Song, Donna Skow, Leslie Martin, Alan David Swinamer, Ming-Hong Hao, John Lord, Zhaoming Xiong, Chris Sarko, Zhulin Tan, Ronald L. Magolda, Christopher Pargellis, Neil Moss, Gao Donghong A, Daniel R. Goldberg, Rachel R. Kroe, Alison Kukulka, Kevin Chungeng Qian, Carol A. Torcellini
Publikováno v:
Journal of medicinal chemistry. 50(17)
Integration of computational methods, X-ray crystallography, and structure-activity relationships will be disclosed, which lead to a new class of p38 inhibitors that bind to p38 MAP kinase in a Phe out conformation.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e7039be517553bebca43f97bb62b4d2
https://pubmed.ncbi.nlm.nih.gov/17658737
https://pubmed.ncbi.nlm.nih.gov/17658737
Autor:
Christopher Ronald Sarko, Antonio J.M. Jr Barbosa, Kevin Chungeng Qian, Mark Stephen Ralph, Neil Moss, Ming-Hong Hao, Daniel R. Goldberg, Tazmeen N. Fadra, Faith Corbo Gaenzler, Fariba Soleymanzadeh, Rachel R. Kroe, Pingrong Liu, Abdelhakim Hammach
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(24)
A new class of benzimidazolone p38 MAP kinase inhibitors was discovered through high-throughput screening. X-ray crystallographic data of the lead molecule with p38 were used to design analogues with improved binding affinity and potency in a cell as
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0981a6403bb9e04689fd0c9d2113d72d
https://pubmed.ncbi.nlm.nih.gov/17010605
https://pubmed.ncbi.nlm.nih.gov/17010605
Autor:
Daniel Kuzmich, Yan Zhang, Jörg Bentzien, Mario G. Cardozo, Raj Betageri, Alison Capolino, Richard M. Nelson, Gerald Nabozny, Zofia Paw, Renee Zindell, Daw-Tsun Shih, Cheng-Kon Shih, David S. Thomson, Ljiljana Zuvela-Jelaska, Kirrane Thomas M, Tazmeen N. Fadra
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(21)
Compound 1, a potent glucocorticoid receptor ligand, contains a quaternary carbon bearing trifluoromethyl and hydroxyl groups. This paper describes the effect of replacing the trifluoromethyl group on binding and agonist activity of the GR ligand 1.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9aa21ffee7079a83841fb713bb048098
https://pubmed.ncbi.nlm.nih.gov/16112571
https://pubmed.ncbi.nlm.nih.gov/16112571
Autor:
Doris Riether, Christian Harcken, Hossein Razavi, Daniel Kuzmich, Thomas Gilmore, JoÌrg Bentzien, Edward J. Pack, Donald Souza, Richard M. Nelson, Alison Kukulka, Tazmeen N. Fadra, Ljiljana Zuvela-Jelaska, Josephine Pelletier, Roger Dinallo, Mark Panzenbeck, Carol Torcellini, Gerald H. Nabozny, David S. Thomson
Publikováno v:
Journal of Medicinal Chemistry; Sep2010, Vol. 53 Issue 18, p6681-6698, 18p