Zobrazeno 1 - 10
of 22
pro vyhledávání: '"David R, Tortolani"'
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:
Ching Kim Tye, Chunhong Yan, Sarah C. Traeger, Wayne Vaccaro, Yingru Zhang, Gerry Everlof, Jianqing Li, Henry Yip, Peng Li, John T. Hunt, Michael A. Poss, Gregory D. Vite, Mussari Christopher P, Steven Sheriff, Asoka Ranasinghe, Haiying Zhang, Richard A. Westhouse, Dharmpal S. Dodd, Richard Rampulla, Zheng Yang, Frank Marsilio, Derek J. Norris, Wen-Ching Han, Tram N. Huynh, Yufen Zhao, Patrice Gill, Nirmala Raghavan, Lalgudi S. Harikrishnan, Ashvinikumar V. Gavai, Susan Wee, John S. Tokarski, Dauh-Rurng Wu, Arvind Mathur, Mei-Li Wen, Huiping Zhang, David R. Tortolani, George V. Delucca, Krista Menard, Francis Y. Lee, Claude A. Quesnelle, Dawn Sun, Vijay T. Ahuja, Daniel O'malley, Christine Huang, Muthoni G. Kamau
Publikováno v:
Journal of Medicinal Chemistry. 64:14247-14265
Inhibition of the bromodomain and extra-terminal (BET) family of adaptor proteins is an attractive strategy for targeting transcriptional regulation of key oncogenes, such as c-MYC. Starting with the screening hit 1, a combination of structure-activi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e6552024d7da4fe4ccaa968fbe1cf079
https://doi.org/10.1021/acs.jmedchem.1c00625
https://doi.org/10.1021/acs.jmedchem.1c00625
Autor:
Dauh-Rurng Wu, Zheng Yang, Steven Sheriff, Muthoni G. Kamau, Lalgudi S. Harikrishnan, Dharmpal S. Dodd, Henry Yip, Christine Huang, Yingru Zhang, Yufen Zhao, Jianqing Li, Richard A. Westhouse, Richard Rampulla, Ashvinikumar V. Gavai, Haiying Zhang, Susan Wee, Dawn Sun, Gerry Everlof, Tram N. Huynh, Ching Su, Derek J. Norris, Arvind Mathur, Wayne Vaccaro, Peng Li, Huiping Zhang, Gregory D. Vite, Mussari Christopher P, John T. Hunt, Asoka Ranasinghe, David R. Tortolani, Nirmala Raghavan, Celia D’Arienzo, Daniel O'malley, Vijay T. Ahuja, Patrice Gill, Lisa Zhang, Claude A. Quesnelle, Tokarski John S, Michael A. Poss
Publikováno v:
Cancer Research. 78:5789-5789
Background: The bromodomains and extra-terminal domain (BET) proteins are a family of 4 adapter proteins, BRD2, BRD3, BRD4, and BRDT, that bind to specific acetylated lysine residues on the histone tails of chromatin and recruit additional proteins t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ad3948219544cdcb29d5e3baea4000aa
https://doi.org/10.1158/1538-7445.am2018-5789
https://doi.org/10.1158/1538-7445.am2018-5789
Autor:
Andrew J. Tebben, Wayne Vaccaro, Xiaoxia Yang, Kim W. McIntyre, Steven Sheriff, Nelly Aranibar, Dharmpal S. Dodd, Stacey Skala, Zheng Yang, Dawn K. Stetsko, Patric M Davis, Theresa Ziemba, Suzanne J. Suchard, Dominique Potin, Karishma Patel, Bang-Chi Chen, Joel C. Barrish, Zili Xiao, Albert J. DelMonte, Scott H. Watterson, Murray McKinnon, David R. Tortolani, Praveen Balimane, Pathanjali Kadiyala, Punit Marathe, Huiping Zhang, Michele Launay, Deborah Lee, ChiehYing Y. Chang, T. G. Murali Dhar
Publikováno v:
Journal of Medicinal Chemistry. 53:3814-3830
Leukocyte function-associated antigen-1 (LFA-1), also known as CD11a/CD18 or alpha(L)beta(2), belongs to the beta(2) integrin subfamily and is constitutively expressed on all leukocytes. The major ligands of LFA-1 include three intercellular adhesion
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f3d21c084dc54390adcd39bb85a2e9b0
https://doi.org/10.1021/jm100348u
https://doi.org/10.1021/jm100348u
Autor:
Johnni Gullo-Brown, Michael A. Poss, Wayne Vaccaro, Tram N. Huynh, Stephanie Barbosa, Carolyn S. Ricca, Mark E. Salvati, Veeraswamy Manne, Zhong Chen, Kenneth J. Leavitt, Soong-Hoon Kim, David R. Tortolani, Donna D. Wei
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:628-632
The synthesis and SAR of a series of pyrrolopyridazine MEK inhibitors are reported. Optimal activity was achieved by incorporation of a 4-phenoxyaniline substituent at C4 and an acylated amine at C6.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c9b1ce0dc69568349a8c7b57436978aa
https://doi.org/10.1016/j.bmcl.2005.10.052
https://doi.org/10.1016/j.bmcl.2005.10.052
Autor:
Scott A. Biller, David R. Tortolani
Publikováno v:
Tetrahedron Letters. 37:5687-5690
A procedure for the preparation of various analogs of miconazole on solid support is described. A novel iodoetherification transformation is utilized as the key synthetic step. This approach has been applied to the combinatorial synthesis of 45 analo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a366799f808db04fb763c9d0c9f96d5a
https://doi.org/10.1016/0040-4039(96)01222-1
https://doi.org/10.1016/0040-4039(96)01222-1
Autor:
Chen-Yi Hung, Michael A. Poss, Steven P. Seitz, Becky Penhallow, George L. Trainor, John S. Tokarski, Wayne Vaccaro, David R. Tortolani, Liqi He, Ricardo M. Attar, Christine M. Tarby, Tai-An Lin
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(18)
A series of aminothiazoles that are potent inhibitors of LIM kinases 1 and 2 is described. Appropriate choice of substituents led to molecules with good selectivity for either enzyme. An advanced member of the series was shown to effectively interfer
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ecabe899a22644c0b9ec6f79e67702ce
https://pubmed.ncbi.nlm.nih.gov/22902653
https://pubmed.ncbi.nlm.nih.gov/22902653
Autor:
John W. Russell, J. E. Jun. Starrett, M. M. Mansuri, Valerie J. Whiterock, John C. Martin, Ismail Ghazzouli, David R. Tortolani, J. M. Hitchcock
Publikováno v:
ChemInform. 25
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e8cabdc971afb369c00b818aa8d3d480
https://doi.org/10.1002/chin.199431267
https://doi.org/10.1002/chin.199431267
Autor:
Valerie J. Whiterock, John W. Russell, John E. Starrett, David R. Tortolani, Michael J. M. Hitchcock, J. C. Martin, Muzammil M. Mansuri
Publikováno v:
ChemInform. 25
A series of phosphonate prodrugs were evaluated in an attempt to increase the oral bioavailability of the anti-HIV agent 9-[2-(phosphonomethoxy)ethyl]adenine (PMEA; 1). The majority of the bis(alkyl ester) and bis(alkyl amide) prodrugs were prepared
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c0d035092ae7bd2c7be8dcd315b8dff9
https://doi.org/10.1002/chin.199444215
https://doi.org/10.1002/chin.199444215
Autor:
Thor Roalsvig, David R. Tortolani, Kuo-Long Yu, Jomary A. Honeyman, Laura Hammer, Patrick G. Spinazze, Peter R. Reczek, Stephen J. Currier, Muzammil M. Mansuri, John E. Starrett, Jacek Ostrowski, Edward J. Pack
Publikováno v:
ChemInform. 27
In search for retinoic acid receptor (RAR) selective ligands, a series of 6-substituted 2-naphthoic acid retinoids were synthesized and evaluated in vitro in a transactivation assay and a competition binding assay for all RARs. These derivatives, in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8f71896cf838c02e0988bf39b26ac888
https://doi.org/10.1002/chin.199638128
https://doi.org/10.1002/chin.199638128