Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Jay P. Theroff"'
Autor:
Deborah Galinis, Sheila J. Miknyoczki, Ted L. Underiner, Damaris Rolon-Steele, Jean Husten, Craig A. Zificsak, Thelma S. Angeles, Torsten Herbertz, Mark S. Albom, Bruce D. Dorsey, Laura S. Kocsis, Kevin J. Wells-Knecht, Jay P. Theroff, Lisa D. Aimone, Kelli S. Zeigler, Candace S. Worrell, Rebecca A. Brown, Christine LoSardo, Seetha Murthy, Jennifer Grobelny
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:660-663
Elaboration of the SAR around a series of 2,4-diaminopyrimidines led to a number of c-Met inhibitors in which kinase selectivity was modulated by substituents appended on the C4-aminobenzamide ring and the nature of the C2-aminoaryl ring. Further lea
Autor:
Maria Emilia Di Francesco, Joseph R. Marszalek, Timothy McAfoos, Christopher L. Carroll, Zhijun Kang, Gang Liu, Jay P. Theroff, Jennifer P. Bardenhager, Madhavi L. Bandi, Jennifer R. Molina, Sonal Gera, Marina Protopopova, Yuting Sun, Mary K. Geck Do, Ningping Feng, Jason P. Gay, Florian Muller, Marina Konopleva, Funda Meric-Bernstam, Carlo Toniatti, Timothy P. Heffernan, Giulio F. Draetta, Philip Jones
Publikováno v:
Cancer Research. 78:1655-1655
Over the past few years we and others reported that specific populations of tumor cells including AML, subsets of lymphoma, glioblastoma, triple negative breast cancer (TNBC), melanoma and pancreatic ductal adenocarcinoma (PDAC) are highly dependent
Autor:
Linda Weinberg, Ted L. Underiner, Mark S. Albom, Craig A. Zificsak, Arup K. Ghose, Renee C. Roemmele, Mangeng Cheng, Karen L. Milkiewicz, Jay P. Theroff, Bruce D. Dorsey, Thelma S. Angeles
Publikováno v:
Bioorganic & Medicinal Chemistry. 18:4351-4362
Dysregulation of the anaplastic lymphoma kinase (ALK) is implicated in a variety of cancers. A series of tetrahydropyrido[2,3-b]pyrazines was constructed as ring-constrained analogs of a known aminopyridine kinase scaffold. Chemistry was developed to
Autor:
Courtney L. Scaife, Craig A. Zificsak, Xuegang Lao, Mark A. Ator, Oana Bollt, Bruce D. Dorsey, Yi Shen, Bruce Ruggeri, Joseph G. Lisko, Jill E. Shea, Jay P. Theroff, Scott K. Kuwada, Xiufen Li
Publikováno v:
Journal of medicinal chemistry. 58(3)
The spread of intra-abdominal cancers is a vexing clinical problem for which there is no widely effective treatment. We discovered previously that (2E)-3-[(4-tert-butylphenyl)sulfonyl]acrylonitrile (1) induced cancer cell apoptosis during adhesion to
Autor:
Philip Jones, M Emilia Di Francesco, Jennifer M. Molina, Marina Protopopova, Madhavi Bandi, Jennifer Bardenhagen, Christopher A. Bristow, Christopher L. Carroll, Ningping Feng, Jason P. Gay, Mary K. Geck Do, Jennifer M. Greer, Marina Konopleva, Zhijun Kang, Gang Liu, Timothy McAfoos, Pietro Morlacchi, Melinda G. Smith, Sonal Fnu, Jay P. Theroff, Giulio Draetta, Carlo Toniatti, Joseph R. Marszalek
Publikováno v:
Clinical Cancer Research. 23:PR01-PR01
Tumor cells normally depend on both glycolysis and oxidative phosphorylation (OXPHOS) to provide the energy and macromolecule building blocks needed to enable continued tumor cell growth. Genetic or epigenetic inactivation of one of these two redunda
Autor:
Ted L. Underiner, Sheryl L. Meyer, Beverly P. Holskin, Thelma S. Angeles, Jay P. Theroff, Jie Qian
Publikováno v:
Assay and drug development technologies. 10(4)
Heat shock protein-90 (HSP90) is an ATP-dependent molecular chaperone with intrinsic ATPase activity. HSP90 is required for the stability and function of client proteins, many of which are involved in oncogenesis. Thus, identification of HSP90 inhibi
Autor:
Joseph G. Lisko, Xuegang Lao, Jay P. Theroff, Yi Shen, Scott K. Kuwada, Craig A. Zificsak, Bruce D. Dorsey, Oana Bollt, Xiufen Li
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(5)
The vast majority of cancer patients die from metastasis, the process by which cancer cells spread to secondary tissues through body fluids. Peritoneal carcinomatosis is a type of metastasis in which cancer cells gain access to the intra-abdominal ca
Autor:
Henry J. Breslin, James P. Finn, Lisa Saville, Jennifer L. Mason, Ted L. Underiner, Derek Dunn, Linda Weinberg, Jean Husten, Mahfuza Jan, Jay P. Theroff, Thelma S. Angeles, Teresa M. O'Kane, Karen L. Milkiewicz, Diane E. Gingrich, Tho V. Thieu, Lisa D. Aimone, Mark S. Albom, Craig A. Zificsak, Bruce D. Dorsey, Pawel Dobrzanski
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(1)
The elaboration of a novel scaffold for the inhibition of JAK2 and FAK kinases was targeted in order to provide a dual inhibitor that could target divergent pathways for tumor cell progression.
Autor:
Mangeng Cheng, Bruce D. Dorsey, Eugen F. Mesaros, Weihua Wan, Matthew R. Quail, Craig A. Zificsak, Mark S. Albom, Gregory R. Ott, Jay P. Theroff, Ted L. Underiner, Thelma S. Angeles, Lisa D. Aimone
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(13)
The incorporation of R,R-1,2-diaminocyclohexane at C4 in a series of 2,4-diaminopyrimidines led to a number of ALK inhibitors in which optimized activity was achieved by conversion of the 2-amino group into a methanesulfonamide. Tumor growth inhibiti
Autor:
Brian Wells, Robert A. Galemo, Dean A. Wacker, Michael J. Orwat, Robert M. Knabb, Ruth R. Wexler, Jeffrey G. Varnes, Steven Bai, Joseph M. Luettgen, Kan He, Jay P. Theroff, Patrick Y.S. Lam, Donald J. P. Pinto
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(2)
Efforts to further optimize the clinical candidate razaxaban have led to a new series of pyrazole-based factor Xa (fXa) inhibitors. Designed to prevent the potential formation of primary aniline metabolites in vivo, the nitrogen of the carboxamido li