Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Nadya Smotrov"'
Autor:
Derun Li, Hongjun Zhang, Hua Zhou, Xuelei Song, Theodore A. Martinot, Prasanthi Geda, Brett A. Hopkins, Jeanine E. Ballard, Stella H. Vincent, Yongxin Han, Nicolas Solban, Karin M. Otte, Mangeng Cheng, J. Richard Miller, Qinglin Pu, Indu Bharathan, Charles A. Lesburg, Ryan D. Cohen, Ian Knemeyer, David Jonathan Bennett, Xavier Fradera, Alfred Lammens, Nadya Smotrov
Publikováno v:
ACS Med Chem Lett
[Image: see text] Herein the discovery of potent IDO1 inhibitors with low predicted human dose is discussed. Metabolite identification (MetID) and structural data were used to strategically incorporate cyclopropane rings into this tetrahydronaphthyri
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83daf5d6fb5e002887daecc8d7be71ff
https://pubmed.ncbi.nlm.nih.gov/34531952
https://pubmed.ncbi.nlm.nih.gov/34531952
Autor:
Kun Liu, Yongxin Han, Nunzio Sciammetta, Chad Chamberlin, Xavier Fradera, Meredeth A. McGowan, Hongjun Zhang, Brett A. Hopkins, J. Richard Miller, Heidi Ferguson, Christine Andrews, Stella H. Vincent, Catherine White, Nadya Smotrov, Omar Mabrouk, Elliott B. Nickbarg, Mangeng Cheng, Amy C. Doty, Prasanthi Geda, Peter Saradjian, Derun Li, Charles A. Lesburg, Xianhai Huang, Pravien Abeywickrema, David L. Sloman, Karin M. Otte, Ian Knemeyer, David Jonathan Bennett, Yongqi Deng, Matthew Richards, Theo Martinot, Patrick J. Curran, Qinglin Pu, Wensheng Yu, Xuelei Song
Publikováno v:
Bioorganicmedicinal chemistry letters. 47
A novel series of IDO1 inhibitors have been identified with good IDO1 Hela cell and human whole blood activity. These inhibitors contain an indoline or a 3-azaindoline scaffold. Their structure-activity-relationship studies have been explored. Compou
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3164872e6af953c66db2580c003d08af
https://pubmed.ncbi.nlm.nih.gov/34166782
https://pubmed.ncbi.nlm.nih.gov/34166782
Autor:
Karin M. Otte, Yongxin Han, Pravien Abeywickrema, Elliott B. Nickbarg, Brett A. Hopkins, Patrick J. Curran, Kun Liu, Chad Chamberlin, Christine Andrews, Mangeng Cheng, Stella H. Vincent, Omar Mabrouk, Matthew Richards, Charles A. Lesburg, Prasanthi Geda, Peter Saradjian, Heidi Ferguson, Alfred Lammens, Sulagna Sanyal, Yongqi Deng, Nunzio Sciammetta, Nadya Smotrov, Ian Knemeyer, Jongwon Lim, Xavier Fradera, J. Richard Miller, Indu Bharathan, Hongjun Zhang, David Jonathan Bennett, Abdelghani Achab, Derun Li, Qinglin Pu, Theodore A. Martinot, Wensheng Yu, Alexander Pasternak, Hua Zhou, Xuelei Song, Peter Spacciapoli, Ryan D. Cohen, Amy C. Doty
Publikováno v:
ACS Med Chem Lett
[Image: see text] Indoleamine-2,3-dioxygenase-1 (IDO1) has emerged as an attractive target for cancer immunotherapy. An automated ligand identification system screen afforded the tetrahydroquinoline class of novel IDO1 inhibitors. Potency and pharmac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7cf6df2b1ea283824056a6ccf880a889
https://europepmc.org/articles/PMC7957919/
https://europepmc.org/articles/PMC7957919/
Autor:
Xavier Fradera, Meredeth A. McGowan, Mangeng Cheng, Pravien Abeywickrema, Karin M. Otte, Prasanthi Geda, Nunzio Sciammetta, Catherine White, Konstanze von Köenig, Charles A. Lesburg, Hyun Chong Woo, Nadya Smotrov, Sarah E Trewick, Patrick J. Curran, Martin Augustin, Christine Andrews, Elizabeth Joshi, Wensheng Yu, Elliott B. Nickbarg, Phillip M. Cowley, Ian Knemeyer, Jongwon Lim, Hua Zhou, Yongxin Han, Xuelei Song, David Jonathan Bennett, Mee Ra Heo, Peter Spacciapoli, J. Richard Miller
Publikováno v:
ACS Med Chem Lett
[Image: see text] Indoleamine-2,3-dioxygenase-1 (IDO1) has emerged as a target of significant interest to the field of cancer immunotherapy, as the upregulation of IDO1 in certain cancers has been linked to host immune evasion and poor prognosis for
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::581b064473f176e3696647f1e7fc716c
https://europepmc.org/articles/PMC7153270/
https://europepmc.org/articles/PMC7153270/
Autor:
Nathaniel L. Elsen, Zangwei Xu, Peter J. Dandliker, Peter Saradjian, Keith W. Rickert, Berengere Sauvagnat, Nadya Smotrov, Dawn L. Hall, Elliott B. Nickbarg, Yiping Chen, Sujata Sharma, Kevin J. Lumb, Maria Kornienko, Noel Byrne, Chad Chamberlin, Christine Andrews, Samantha J Allen, Ilona Kariv, Jennifer M. Shipman, Patrick J. Curran, Kevin G. Coleman, Beutel Bruce A, Rachael E. Ford, Victoria Kutilek, Andrew Hashke, Rafael Fernandez, Tianxiao Sun, Matthew Richards, Ryan Boinay
Publikováno v:
SLAS Discovery. 21:608-619
The primary objective of early drug discovery is to associate druggable target space with a desired phenotype. The inability to efficiently associate these often leads to failure early in the drug discovery process. In this proof-of-concept study, th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::321009edd98ca17a57d26928e293e5e3
https://doi.org/10.1177/1087057116637353
https://doi.org/10.1177/1087057116637353
Autor:
Hugh Nuthall, Lily Y. Moy, Candia M. Kenific, Sean P. Ahearn, Damaris Diaz, Elizabeth Helen Kelley, Bethany Hughes, Armetta D. Hill, Adam J. Schell, Nadya Smotrov, Valentina V. Jeliazkova-Mecheva, Chris Moxham, Hua Zhou, Sanjiv J. Shah, Andrew Rosenau, Alexey Rivkin, Sam Kattar, Joey L. Methot, Richard G. Ball, William Brown, Mark S. Shearman, Chaomin Li, Christian Fischer, Alexander A. Szewczak, Sujal V. Deshmukh, Dawn M. Mampreian, Thomas A. Miller, Benito Munoz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:3495-3500
The triazolyl amide γ-secretase modulators are potent alternatives to the cinnamyl amides that have entered the clinic for the treatment of Alzheimer's disease. Herein we build on the lead benzoazepinones described in our prior communication with im
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a00409b5294ccf9d203089fa0df9362
https://doi.org/10.1016/j.bmcl.2015.06.032
https://doi.org/10.1016/j.bmcl.2015.06.032
Autor:
Sujal V. Deshmukh, Susan L. Zultanski, George N. Nikov, Christopher M. Moxham, Armetta D. Hill, Lily Y. Moy, Nadya Smotrov, Christian Fischer, Hua Zhou, Joey L. Methot, Maria S. Michener, Bethany Hughes, Damaris Diaz, Zhenhua Wu, Jacquelynn J. Cook, Sanjiv J. Shah, Benito Munoz, Jonathan C. Cruz, Flobert Tanga, Nathan Bays, Melanie Bouthillette, Bo-Sheng Pan, Valentina V. Jeliazkova-Mecheva, Ikuo Hayashi, Mark S. Shearman, Candia M. Kenific, Deborah Walker
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(17)
Synthesis and SAR studies of novel triazolobenzazepinones as gamma secretase modulators (GSMs) are presented in this communication. Starting from our azepinone leads, optimization studies toward improving central lowering of Aβ42 led to the discover
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0acca6592ca6102565f303c9312bd5b
https://pubmed.ncbi.nlm.nih.gov/26212776
https://pubmed.ncbi.nlm.nih.gov/26212776
Autor:
George N. Nikov, Flobert Tanga, Chris Moxham, Ziping Yang, Chaomin Li, Richard G. Ball, Joshua Close, Richard W. Heidebrecht, Gloria Y. Kwei, Lin Xu, Laura Surdi, Xiaoliu Geng, Candia Kenefic, Sanjiv J. Shah, Dan F. Savage, Valentina V. Jeliazkova-Mecheva, Jennifer Chapnick, Julie Elizabeth Burke, Solomon Kattar, Bethany Hughes, Lily Y. Moy, Sujal V. Deshmukh, Paul Moses, Damaris Diaz, John Kevin Leach, Paul Tempest, John Hendrix, Amanda Markarewicz, Nadya Smotrov, Ilona Kariv, Michael J. McNevin, Ben Munoz, Mark S. Shearman, Thomas A. Miller
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(9)
Alzheimer’s disease is a major unmet medical need with pathology characterized by extracellular proteinaceous plaques comprised primarily of β-amyloid. γ-Secretase is a critical enzyme in the cellular pathway responsible for the formation of a ra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d76db0c66a4f7b201b3015ad1e1e6a7
https://pubmed.ncbi.nlm.nih.gov/22483609
https://pubmed.ncbi.nlm.nih.gov/22483609
Publikováno v:
Journal of biomolecular screening. 14(4)
c-Met is a receptor tyrosine kinase (RTK) with a critical role in many fundamental cellular processes, including cell proliferation and differentiation. Deregulated c-Met signaling has been implicated in both the initiation and progression of human c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f41934e775a841ef463b1e56da2f165a
https://pubmed.ncbi.nlm.nih.gov/19403923
https://pubmed.ncbi.nlm.nih.gov/19403923