Zobrazeno 1 - 10
of 92
pro vyhledávání: '"Robert M, Borzilleri"'
Autor:
Matthew T. Villaume, Eran Sella, Garrett Saul, Robert M. Borzilleri, Joseph Fargnoli, Kathy A. Johnston, Haiying Zhang, Mark P. Fereshteh, T. G. Murali Dhar, Phil S. Baran
Publikováno v:
ACS Central Science, Vol 2, Iss 1, Pp 27-31 (2015)
Externí odkaz:
https://doaj.org/article/0458d0a0756d44d3b690b8d081d19332
Autor:
Shiuhang Yip, Emily Luk, Anwar Murtaza, Yong Zhang, Michael A. Poss, Louis J. Lombardo, Nimmi Raghavan, Zheng Yang, James Kempson, Audris Huang, David R. Tortolani, Jesse Swanson, Xiaoping Hou, Joseph Pawluczyk, James Smalley, Honghe Wan, Karen E. Parrish, Robert M. Borzilleri, Ashok V. Purandare, Karen Augustine-Rauch, Andrew F. Donnell
Publikováno v:
Journal of Medicinal Chemistry. 64:15787-15798
Inhibition of TGFβ signaling in concert with a checkpoint blockade has been shown to provide improved and durable antitumor immune response in mouse models. However, on-target adverse cardiovascular effects have limited the clinical use of TGFβ rec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aebde71751ab18259045cb79ccd54677
https://doi.org/10.1021/acs.jmedchem.0c02043
https://doi.org/10.1021/acs.jmedchem.0c02043
Autor:
Liping Zhang, James Kempson, Anuradha Gupta, Pirama Nayagam Arunachalam, Yoganand Shanmugam, Suresh Krishnamoorthy, Prakasam Kuppusamy, Zhenqiu Hong, Cherney Emily Charlotte, Richard R. Rampulla, Roshan Y. Nimje, Duraisamy Ramasamy, Aaron Balog, Robert M. Borzilleri, Arvind Mathur, Haridhas Manoharan
Publikováno v:
Organic Process Research & Development. 25:1680-1689
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3c7b59382a9f923a409405a406bda275
https://doi.org/10.1021/acs.oprd.1c00142
https://doi.org/10.1021/acs.oprd.1c00142
Autor:
Jonathan Lippy, Robert M. Borzilleri, Andrew J. Tebben, Litao Zhang, Charu Chaudhry, William J. Pitts, John S. Tokarski
Publikováno v:
Drug Discovery Today. 26:1115-1125
Kinases, accounting for 20% of the human genome, have been the focus of pharmaceutical drug discovery efforts for over three decades. Despite concerns surrounding the tractability of kinases as drug targets, it is evident that kinase drug discovery o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a1427877b39cb9b4aab8094dddf3cf4
https://doi.org/10.1016/j.drudis.2021.01.018
https://doi.org/10.1016/j.drudis.2021.01.018
Autor:
Aberra Fura, Shiuhang Yip, Georgia Cornelius, Hai-Yun Xiao, Qingjie Liu, Sha Li, Ning Li, Nicholas A. Meanwell, Shailesh Dudhgaonkar, Max Ruzanov, Jenny Xie, Zili Xiao, Purnima Khandelwal, Carolyn A. Weigelt, David J. Shuster, Dauh-Rurng Wu, T. G. Murali Dhar, Tara Sherry, Yang Michael G, Kevin Stefanski, Jignesh Nagar, Rex Denton, Qihong Zhao, Peng Li, Silvi A. Chacko, Arun Govindarajan, Robert M. Borzilleri, John S. Sack, Yeheng Zhu, Yunling Song, Dawn Sun, Anjuman Rudra, Mary T. Obermeier, Jinhong Wang, Douglas G. Batt, Venkata Murali
Publikováno v:
ACS Med Chem Lett
[Image: see text] Structure–activity relationship studies directed toward the replacement of the fused phenyl ring of the lead hexahydrobenzoindole RORγt inverse agonist series represented by 1 with heterocyclic moieties led to the identification
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3296d470de82e26da82050921646783
https://doi.org/10.1021/acsmedchemlett.1c00112
https://doi.org/10.1021/acsmedchemlett.1c00112
Publikováno v:
Burger's Medicinal Chemistry and Drug Discovery. :1-86
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::346314e8fd3ddb9cb747245e50d6ae4f
https://doi.org/10.1002/0471266949.bmc279
https://doi.org/10.1002/0471266949.bmc279
Autor:
Mark Fereshteh, Xiao Zhu, Tai-An Lin, Prabhakar Rajanna, Cherney Emily Charlotte, Aravind Anandam, Xin Li, Derrick Maley, Liping Zhang, Gopal Dhar, Aaron Balog, Robert M. Borzilleri, Johnni Gullo-Brown, T. Thanga Mariappan, Kathy Johnston-Allegretto, Christine Huang, Venkata Murali, John T. Hunt, Sandeep Mahankali, Gregory D. Vite, Lisa M. Kopcho, Shweta Padmanabhan, Sarah C. Traeger
Publikováno v:
ACS Med Chem Lett
[Image: see text] Indoleamine 2,3-dioxygenase 1 (IDO1) has been identified as a target for small-molecule immunotherapy for the treatment of a variety of cancers including renal cell carcinoma and metastatic melanoma. This work focuses on the identif
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c69bf6be584624b416a38e3f63d582b0
https://doi.org/10.1021/acsmedchemlett.1c00014
https://doi.org/10.1021/acsmedchemlett.1c00014
Autor:
Emily Luk, Karen E. Parrish, Yue-Zhong Shu, Anwar Murtaza, Yongnian Sun, Jinwen Huang, Robert M. Borzilleri, Paul Stetsko, Mary Ellen Cvijic, Jonathan G. Pabalan, Lihong Cheng, Zheng Yang, Jesse Swanson, James R. Burke, Tatyana Zvyaga, James Smalley, Karen A. Augustine
Publikováno v:
Biopharmaceutics & Drug Disposition. 42:137-149
Transforming growth factor beta (TGF-β) is a pleiotropic cytokine that has a wide array of biological effects. For decades, tumor biology implicated TGF-β as an attractive therapeutic target due to its immunosuppressive effects. Toward this end, mu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e12c605d2321e62c539be94c50fc986d
https://doi.org/10.1002/bdd.2256
https://doi.org/10.1002/bdd.2256
Autor:
David K. Leahy, Martin D. Eastgate, Arvind Mathur, Richard Rampulla, Varadharajan Subramanian, Upender Velaparthi, Sathishkumar Chandrasekaran, Karthikeyan Chinnakalai, Arun Kumar Gupta, Antony Savarimuthu, Thirumalai Lakshminarasimhan, Souvik Rakshit, Indasi Gopikumar, Jayakumar Sankara Warrier, Chetan Padmakar Darne, Robert M. Borzilleri, Rajappa Vaidyanathan, Anuradha Gupta, Ananta Karmakar, Vignesh Radhakrishnan, Muthalagu Vetrichelvan, Dyamanna Doddalingappa, Senthil Palani
Publikováno v:
Organic Process Research & Development. 24:1310-1320
A scalable route to the small molecule TGFβR1 inhibitor BMS-986260 (1) was developed. This alternative approach circumvented the purification of intermediates by column chromatography and provided ...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c1479cf30ab1db39b487237c60ba0c40
https://doi.org/10.1021/acs.oprd.0c00232
https://doi.org/10.1021/acs.oprd.0c00232
Autor:
Jennifer Brown, Karen E. Parrish, Andrew J. Tebben, Jonathan Lippy, Kamalavenkatesh Palanisamy, Todd Kinsella, Chetan Padmakar Darne, Vinay K. Holenarsipur, Anwar Murtaza, Muthalagu Vetrichelvan, Chunhong Yan, Karen Augustine-Rauch, Max Ruzanov, Mark Fereshteh, Upender Velaparthi, Gopal Dhar, Gregory D. Vite, Peiying Liu, Steven Sheriff, Jayakumar Sankara Warrier, Aravind Anandam, Marina Gelman, Arvind Mathur, Barri Wautlet, Robert M. Borzilleri, Hasibur Rahaman, Zheng Yang, Anuradha Gupta, Arun Kumar Gupta, Rajinder Singh, Joseph Fargnoli, Jesse Swanson
Publikováno v:
ACS Med Chem Lett
[Image: see text] Novel imidazole-based TGFβR1 inhibitors were identified and optimized for potency, selectivity, and pharmacokinetic and physicochemical characteristics. Herein, we report the discovery, optimization, and evaluation of a potent, sel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57c0a6b7db9a564a606d22c0c365bdb7
https://doi.org/10.1021/acsmedchemlett.9b00552
https://doi.org/10.1021/acsmedchemlett.9b00552