Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Qinglin Pu"'
Autor:
Anandan Palani, Matthew Lloyd Childers, Qinglin Pu, Matthew J. Mitcheltree, Symon Gathiaka, Christian Fischer, Lisa Nogle, Rachel L. Palte, Jared N. Cumming, J. Richard Miller, Spencer McMinn, Hai-Young Kim, Hongjun Zhang, Charles A. Lesburg, Adam Beard, Donovon A. Adpressa, Josep Saurí, Derun Li, Theodore A. Martinot, Thomas W. Lyons, David L. Sloman, Jialiang Wang, Peter Spacciapoli, Min Lu, Abdelghani Achab
Publikováno v:
ACS Med Chem Lett
[Image: see text] Comprehensive synthetic strategies afforded a diverse set of structurally unique bicyclic proline-containing arginase inhibitors with a high degree of three-dimensionality. The analogs that favored the Cγ-exo conformation of the pr
Autor:
Derun Li, David L. Sloman, Abdelghani Achab, Hua Zhou, Meredeth A. McGowan, Catherine White, Craig Gibeau, Hongjun Zhang, Qinglin Pu, Indu Bharathan, Brett Hopkins, Kun Liu, Heidi Ferguson, Xavier Fradera, Charles A. Lesburg, Theodore A. Martinot, Ji Qi, Zhiguo J. Song, Jingjun Yin, Huangguang Zhang, Licheng Song, Baoqiang Wan, Suzanne DAddio, Nicolas Solban, J. Richard Miller, Beata Zamlynny, Alan Bass, Elizabeth Freeland, Bridget Ykoruk, Catherine Hilliard, Jude Ferraro, Jin Zhai, Ian Knemeyer, Karin M. Otte, Stella Vincent, Nunzio Sciammetta, Alexander Pasternak, David Jonathan Bennett, Yongxin Han
Publikováno v:
Journal of medicinal chemistry. 65(8)
3,3-Disubstituted oxetanes have been utilized as bioisosteres for gem-dimethyl and cyclobutane functionalities. We report the discovery of a novel class of oxetane indole-amine 2,3-dioxygenase (IDO1) inhibitors suitable for Q3W (once every 3 weeks) o
Autor:
Nicolas Solban, Alexander Pasternak, Qinglin Pu, Amy C. Doty, David Jonathan Bennett, Charles A. Lesburg, Wensheng Yu, Prasanthi Geda, Nunzio Sciammetta, J. Richard Miller, Hua Zhou, Xuelei Song, Yongxin Han, Lars Neumann, David L. Sloman, Mangeng Cheng, Heidi Ferguson, Karin M. Otte, Liangqin Guo, Hongjun Zhang, Alfred Lammens, Xavier Fradera, Meredeth A. McGowan
Publikováno v:
ACS Med Chem Lett
[Image: see text] Indoleamine-2,3-dioxygenase 1 (IDO1) inhibition and its combination with immune checkpoint inhibitors like pembrolizumab have drawn considerable attention from both academia and the pharmaceutical industry. Here, we describe the dis
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
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
Autor:
Theodore A. Martinot, Xavier Fradera, Meredeth A. McGowan, Wensheng Yu, Heidi Ferguson, Purakattle J Biju, H. Zhou, Nicolas Solban, Qinglin Pu, Yongxin Han, Xiao Wang, Kun Liu, Ravi Kurukulasuriya, Yu-hong Lam, Abdelghani Achab, Karin M. Otte, Michael J. Ardolino, Amy C. Doty, Charles A. Lesburg, J. Richard Miller, Yongqi Deng, Mangeng Cheng, Hongjun Zhang, Ian Knemeyer, Nunzio Sciammetta, David Jonathan Bennett
Publikováno v:
ACS Med Chem Lett
[Image: see text] Checkpoint inhibitors have demonstrated unprecedented efficacy and are evolving to become standard of care for certain types of cancers. However, low overall response rates often hamper the broad utility and potential of these break
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:
Anand Palani, Min Lu, Jennifer O'Neil, Christopher Brynczka, Lisa Nogle, Amy C. Doty, Christian Fischer, Hai-Young Kim, Abdelghani Achab, Adam Beard, Nicole C. Walsh, Matthew Lloyd Childers, Kalyan Chakravarthy, Josep Saurí, Amy D. DeCastro, Peter W. Fan, Qinglin Pu, Richard A. Miller, Matthew J. Mitcheltree, Rachel L. Palte, Theodore A. Martinot, Hongjun Zhang, Symon Gathiaka, Roshi Afshar, Thomas W. Lyons, Spencer McMinn, Mangeng Cheng, Derun Li
Publikováno v:
Cancer Research. 81:297-297
Arginase overexpression has been associated with poor survival rates in advanced cancer patients treated with Keytruda. High levels of Arginase may lead to a depletion of arginine within the tumor microenvironment, inhibiting the immune response. Thu
Autor:
Derun Li, Hongjun Zhang, Lyons, Thomas W., Min Lu, Achab, Abdelghani, Qinglin Pu, Childers, Matthew, Mitcheltree, Matthew J., Jialiang Wang, Martinot, Theodore A., McMinn, Spencer E., Sloman, David L., Palani, Anandan, Beard, Adam, Nogle, Lisa, Gathiaka, Symon, Saurí, Josep, Hai-Young Kim, Adpressa, Donovon, Spacciapoli, Peter
Publikováno v:
ACS Medicinal Chemistry Letters; 11/11/2021, Vol. 12 Issue 11, p1678-1688, 11p
Autor:
Kamil Paruch, Timothy J. Guzi, Ruichao Shen, Marc A. Labroli, Judson E. Richard, Michael P. Dwyer, Kristen E. Rosner, Janeta Popovici-Muller, Qinglin Pu
Publikováno v:
Tetrahedron Letters. 55:598-602
A novel class of 5-amino-2,5-dideoxy-2,2-difluorocytidine derivatives has been synthesized in order to identify anticancer nucleoside analogs. Several synthetic routes were devised and implemented which relied upon either SN2 displacement or reductiv