Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Kevin J. Curran"'
Autor:
Michelle L. Hermiston, Christina Baggott, A. Yasemin Goksenin, Michael Kunicki, Julie-An Talano, Theodore W. Laetsch, Steven P. Margossian, Michael R. Verneris, Christine L Phillips, Crystal L. Mackall, Vasant Chinnabhandar, Prakash Satwani, Kevin J. Curran, Nicole Karras, Liora M. Schultz, Heather E. Stefanski, Snehit Prabhu, Muna Qayed, Patrick A. Brown, Amy K. Keating, Amy Moskop, Jenna Rossoff, Christa Krupski, Cara A Rabik, Vanessa A Fabrizio, Holly L Pacenta, Rachel Wilcox, G.D. Myers
Publikováno v:
Blood. 136:14-15
Introduction: Chimeric Antigen Receptor (CAR) T cell therapy targeting CD19 has shifted our treatment approach for relapsed and refractory (r/r) pediatric B cell acute lymphoblastic leukemia (ALL). The landmark ELIANA pediatric trial studying tisagen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2648-2653
Isosteric replacement of one of the 3,5-ethylene-bridged morpholines in 2-arylureidophenyl-4,6-di(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines led to significant improvements in human microsomal stability. 3-R-Me-morpholine and tetrahydropyran were
Autor:
Judy Lucas, Ker Yu, Kevin J. Curran, David J. Richard, Lourdes Toral-Barza, Jeroen C. Verheijen, Joshua Kaplan, Irwin Hollander, Arie Zask
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2644-2647
Incorporation of bridged morpholines in monocyclic triazine PI3K/mTOR inhibitors gave compounds with increased mTOR selectivity relative to the corresponding morpholine analogs. Compounds with ureidophenyl groups gave highly potent and selective mTOR
Autor:
Arie Zask, Lourdes Toral-Barza, Jeroen C. Verheijen, Natasja Brooijmans, David J. Richard, Semiramis Ayral-Kaloustian, Ker Yu, Kevin J. Curran, Joshua Kaplan, Irwin Hollander, Eric M. Bennett
Publikováno v:
Journal of Medicinal Chemistry. 52:7942-7945
Dramatic improvements in mTOR-targeting selectivity were achieved by replacing morpholine in pyrazolopyrimidine inhibitors with bridged morpholines. Analogues with subnanomolar mTOR IC(50) values and up to 26000-fold selectivity versus PI3Kalpha were
Autor:
Kevin J. Curran, Boris Feld, Amar S. Prashad, Anita Y. M. Howe, John O'Connell, Martin Joseph Digrandi, Atul Agarwal, Alan G. Sutherland, Bloom Jonathan David, Bernard Dean Johnson, Thomas Nittoli, Shabana Insaf, Rajiv Chopra, Mark Orlowski, Karen L. Wheless, M. Brawner Floyd, Tarek S. Mansour
Publikováno v:
Journal of Medicinal Chemistry. 50:2108-2116
A series of potent anthranilic acid-based inhibitors of the hepatitis C NS5B polymerase has been identified. The inhibitors bind to a site on NS5B between the thumb and palm regions adjacent to the active site as determined by X-ray crystallography o
Autor:
John O'Connell, Kevin J. Curran, Kristine Svenson, Anita Y. M. Howe, Kitae Lim, Steven F. Sukits, Mengxiao Shi, Ariamala Gopalsamy, Boris Feld, Girija Krishnamurthy, Rajiv Chopra, Tarek S. Mansour, Atul Agarwal, Mark Orlowski, Joel Bard, John W. Ellingboe, Gregory Ciszewski
Publikováno v:
Journal of Medicinal Chemistry. 49:3052-3055
Through high throughput screening, substituted proline sulfonamide 6 was identified as HCV NS5b RNA-dependent RNA polymerase inhibitor. Optimization of various regions of the lead molecule resulted in compounds that displayed good potency and selecti
Autor:
Boris Feld, Emily B. Norton, Russell Dushin, Kevin J. Curran, Ross Adma Antonia, Stanley A. Lang, Terefenko Eugene Anthony, Martin Joseph Digrandi, Thomas R. Jones, Bloom Jonathan David, Fran Donahue
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:3401-3406
A series of highly potent thiourea inhibitors of cytomegalovirus (CMV) with improved stability properties was prepared and evaluated. Compound 29 inhibited the virus in cultured HFF cells with IC50 of 0.2 nM.
Autor:
Kevin J. Curran, Judy Lucas, David J. Richard, Arie Zask, Ker Yu, Joshua Kaplan, Semiramis Ayral-Kaloustian, Jeroen C. Verheijen, Lourdes Toral-Barza, Irwin Hollander
Publikováno v:
ChemInform. 41
A series of pyrazolopyrimidine mammalian Target Of Rapamycin (mTOR) inhibitors with various substituents at the 1-position have been prepared, resulting in compounds with excellent potency, selectivity and microsomal stability. Combination of a 1-cyc
Autor:
Judy Lucas, Irwin Hollander, Joshua Kaplan, Lourdes Toral-Barza, Arie Zask, Kevin J. Curran, David J. Richard, Ker Yu, Semiramis Ayral-Kaloustian, Jeroen C. Verheijen
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(4)
A series of pyrazolopyrimidine mammalian Target Of Rapamycin (mTOR) inhibitors with various substituents at the 1-position have been prepared, resulting in compounds with excellent potency, selectivity and microsomal stability. Combination of a 1-cyc
Autor:
Kevin J. Curran, Jeroen C. Verheijen, Judy Lucas, Lourdes Toral-Barza, Joshua Kaplan, David J. Richard, Irwin Hollander, Arie Zask, Ker Yu
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(24)
A series of highly potent and selective pyrazolopyrimidine mTOR inhibitors which contain water-solubilizing groups attached to the 6-arylureidophenyl moiety have been prepared. Such derivatives displayed superior potency to those in which these appen