Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Tram N. Huynh"'
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:
Johnson Walter Lewis, Sung Mei-Chen, Daniel Menezes, Chin Pan, Gregory D. Vite, Yong Zhang, Shrikant Deshpande, Vangipuram S. Rangan, Madhura Deshpande, Richard Rampulla, Ganapathy Sarma, Prasanna Sivaprakasam, Arvind Rajpal, David R. Langley, Tram N. Huynh, Arvind Mathur, Ivar M. McDonald, Naidu S. Chowdari, Pina M. Cardarelli, Bethanne M. Warrack, Srikanth Kotapati, Yichong Wang, Chetana Rao, David Passmore, Robert A. Mate, Robert M. Borzilleri, Sanjeev Gangwar
Publikováno v:
Journal of medicinal chemistry. 63(22)
A series of tetrahydroisoquinoline-based benzodiazepine dimers were synthesized and tested for in vitro cytotoxicity against a panel of cancer cell lines. Structure-activity relationship investigation of various spacers guided by molecular modeling s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c92a9ea42e85c4d5cf7895d4d3aa6edc
https://pubmed.ncbi.nlm.nih.gov/33155811
https://pubmed.ncbi.nlm.nih.gov/33155811
Autor:
Yanling Huang, Jingwu Duan, Carolyn A. Weigelt, Cullen L. Cavallaro, Javed Khan, Brian E. Fink, Muthoni G. Kamau, Zheming Ruan, Lan-Ying Qin, Sylwia Stachura, Cliff Chen, Murali Gururajan, Lalgudi S. Harikrishnan, Tram N. Huynh, John S. Sack, Anwar Murtaza, Daniel O'malley, Zhuyin Li, Melissa Yarde, Max Ruzanov, Virna Borowski, Patrice Gill, Huadong Sun, Zhonghui Lu, Jessica J. Wong
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(12)
Substituted benzyloxy aryl compound 2 was identified as an RORγt agonist. Structure based drug design efforts resulted in a potent and selective tricyclic compound 19 which, when administered orally in an MC38 mouse tumor model, demonstrated a desir
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d28391368dbe9fe0275182d85ed69ba6
https://pubmed.ncbi.nlm.nih.gov/32334911
https://pubmed.ncbi.nlm.nih.gov/32334911
Autor:
Robert M. Townsend, Hai Yun Xiao, Joel C. Barrish, Sium Habte, Arthur M. Doweyko, Steven G. Nadler, Hua Gong, Bingwei V. Yang, John H. Dodd, Tram N. Huynh, John E. Somerville, Mark D. Cunningham, Lorraine I. McKay, David J. Shuster, Michele McMahon, David S. Weinstein, Lidia M. Doweyko, Wayne Vaccaro, Deborah A. Holloway
Publikováno v:
Journal of Medicinal Chemistry. 53:8241-8251
A series of 2,2-dimethyl-3,3-diphenyl-propanamides as novel glucocorticoid receptor modulators is reported. SAR exploration led to the identification of 4-hydroxyphenyl propanamide derivatives displaying good agonist activity in GR-mediated transrepr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e18337b275f845f960a3b529ed7e13f
https://doi.org/10.1021/jm100957a
https://doi.org/10.1021/jm100957a
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:
Matthew V. Lorenzi, Wayne Vaccaro, Marco M. Gottardis, Simona Bindi, Michael A. Poss, Sandrine Thieffine, George L. Trainor, Lata Jayaraman, Paola Vianello, Fulvia Roletto, Ashok V. Purandare, Suhong Pang, Zhong Chen, Tram N. Huynh, Arturo Galvani, Jieping Geng, Tiziano Bandiera
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2924-2927
Design, synthesis, and SAR development led to the identification of the potent, novel, and selective pyrazole based inhibitor (7f) of Coactivator Associated Arginine Methyltransferase (CARM1).
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::769baa6101ece04febd20a1b6b99029b
https://doi.org/10.1016/j.bmcl.2009.04.075
https://doi.org/10.1016/j.bmcl.2009.04.075
Autor:
Suhong Pang, Michael A. Poss, Zhong Chen, Ashok V. Purandare, Kimberly Nowak, Wayne Vaccaro, Tram N. Huynh, Jieping Geng, Lata Jayaraman, Jonathan O’Connell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4438-4441
This study reports the identification and Hits to Leads optimization of inhibitors of coactivator associated arginine methyltransferase (CARM1). Compound 7b is a potent, selective inhibitor of CARM1.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6375662ab0011ae5845d84112c937b80
https://doi.org/10.1016/j.bmcl.2008.06.026
https://doi.org/10.1016/j.bmcl.2008.06.026
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:
John H. Dodd, Katerina Leftheris, William J. Pitts, Michael A. Poss, Joel C. Barrish, Gary C. Starling, Andrew Watson, Peter A. Kiener, Wayne Vaccaro, Junqing Guo, Tram N. Huynh, Baerbel R. Brown, Karen L. Donaldson, Jacques Y. Roberge, Joseph Barbosa
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:2955-2958
A series of purine based inhibitors of PDE7 has been derived from screening lead 1a. The synthesis, structure-activity relationships (SAR), and selectivity against several other PDE family members are described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b6f6a1c267658672e5c5ac6f75f2b584
https://doi.org/10.1016/j.bmcl.2004.03.021
https://doi.org/10.1016/j.bmcl.2004.03.021
Autor:
Huabin Sun, Joseph Prol, Karnail S. Atwal, T.W. Harper, Yolanda Caringal, Michael A. Blanar, Ruth R. Wexler, Jinping Gan, Christine Huang, Wayne Vaccaro, Alexander Kover, Paul Levesque, Heather Finlay, Lin Yan, John Lloyd, John D. Dimarco, Mary Lee Conder, Tram N. Huynh, Bhandaru Rao S, Gauri Bhave
Publikováno v:
Journal of medicinal chemistry. 55(7)
Previously disclosed dihydropyrazolopyrimidines are potent and selective blockers of I(Kur) current. A potential liability with this chemotype is the formation of a reactive metabolite which demonstrated covalent binding to protein in vitro. When sub
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::839ac692afc55a7651f54a83a704a341
https://pubmed.ncbi.nlm.nih.gov/22409629
https://pubmed.ncbi.nlm.nih.gov/22409629