Zobrazeno 1 - 10
of 52
pro vyhledávání: '"Mark D. Wittman"'
Autor:
John Morrison, Steven Sheriff, Mark D. Wittman, Gregory A. Locke, Bradley C. Pearce, Erika M. V. Araujo, Andrew P. Degnan, Christopher W. Allard, Dan You, Xin Li, Kurt Zimmermann, Anwar Murtaza, Benjamin M. Johnson, Caitlyn Stromko, Jinqi Liu, Gregory D. Vite, Godwin Kwame Kumi, Karen E. Parrish, Alan Futran, Johnson Walter Lewis
Publikováno v:
ACS Medicinal Chemistry Letters
While the discovery of immune checkpoint inhibitors has led to robust, durable responses in a range of cancers, many patients do not respond to currently available therapeutics. Therefore, an urgent need exists to identify alternative mechanisms to a
Autor:
Stephen Hillerman, Andrew P. Degnan, Benjamin M. Johnson, Yi Fan, Elizabeth Duperret, Dandan Zhao, Jinqi Liu, John T. Hunt, John Morrison, Rajarshi Bhadra, Luisa Salter-Cid, Charu Chaudhry, Karen E. Parrish, Jennifer Koenitzer, Stephanie W. Briceno, Joshua Curtin, John N. Feder, Caitlyn Stromko, Emma Lees, Dan You, Anwar Murtaza, Michael Quigley, Gregory A. Locke, Mark D. Wittman, Giridharan Gokulrangan, Yali Chen, Chan Gao, Godwin Kwame Kumi, Miguel Sanjuan, Johnni Gullo-Brown
Publikováno v:
Journal for ImmunoTherapy of Cancer, Vol 9, Iss 1 (2021)
Journal for Immunotherapy of Cancer
Journal for Immunotherapy of Cancer
BackgroundHematopoietic progenitor kinase 1 (HPK1 or MAP4K1) has been demonstrated as a negative intracellular immune checkpoint in mediating antitumor immunity in studies with HPK1 knockout and kinase dead mice. Pharmacological inhibition of HPK1 is
Autor:
Dolatrai M. Vyas, Krista Menard, Joan M. Carboni, David B. Frennesson, Marco M. Gottardis, Kurt Zimmermann, Ann Greer, Upender Velaparthi, Francis Y. Lee, Saulnier Mark G, Peiying Liu, George L. Trainor, Aixin Li, Mark D. Wittman, Wendy Clarke, Zheng Yang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3182-3185
A series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one were synthesized to modulate CYP3A4 inhibition and improve aqueous solubility of our prototypical compound BMS-536924 (1), while maintaining potent IGF-1
Autor:
Joan M. Carboni, David R. Langley, Upender Velaparthi, Aixin Li, Saulnier Mark G, Ann Greer, Kurt Zimmermann, Xiaopeng Sang, Zheng Yang, Mark D. Wittman, Ricardo M. Attar, Lorell Discenza, Dolatrai M. Vyas, Praveen Balimane, Marco M. Gottardis, David B. Frennesson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4075-4080
3-(Benzimidazol-2-yl)-pyridine-2-one-based ATP competitive inhibitors of Insulin-like Growth Factor 1 Kinase (IGF-IR) were optimized for reduced Cyp3A4 inhibition and improved oral exposure. The use of malonate as methyl anion synthon via S(N)Ar reac
Autor:
Joan M. Carboni, Aixin Li, Dolatrai M. Vyas, Marco M. Gottardis, Ricardo M. Attar, Upender Velaparthi, Peiying Liu, Mark D. Wittman, Ann Greer, Zoeckler Mary Edson, Balu Balasubramanian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3072-3076
A series of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) were examined in which the pendant imidazole moiety was replaced to improve selectivity for IGF-1R inhibition over cytochrome P450
Autor:
Peiying Liu, Yax Sun, Xiaopeng Sang, Upender Velaparthi, Joan M. Carboni, Ann Greer, Dolatrai M. Vyas, Ricardo M. Attar, David R. Langley, ChiehYing Y. Chang, Stoffan Karen M, Kurt Zimmermann, Aixin Li, Balu Balasubramanian, Mark D. Wittman, John S. Sack, Bruce L. Jacobsen, Marco M. Gottardis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2317-2321
The discovery and synthesis of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor 1-receptor (IGF-1R) are presented. Installing amine containing side chains at the 4-position of pyridone ring significantly improved
Autor:
Ann Greer, Stoffan Karen M, Joan M. Carboni, Bruce L. Jacobson, Zoeckler Mary Edson, Marco M. Gottardis, Dolatrai M. Vyas, Ricardo M. Attar, Aixin Li, Steven Hansel, Subramaniam Krishnanathan, Mark D. Wittman, Pieying Liu, Chiehying Chang, Yax Sun, Upender Velaparthi, Balu Balasubramanian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:974-977
A novel class of 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase is described. This report discusses the SAR of 4-(2-hydroxy-2-phenylethylamino)-substituted pyridones with improved IGF-1R potency.
Autor:
Cindy Wang, Joan M. Carboni, Marco M. Gottardis, Ann Greer, David Bol, Amy Camuso, Aixin Li, Bruce Rowley, Warren Hurlburt, Brent A. Rupnow, Francis Y.F. Lee, Darryl L. Hadsell, Mark D. Wittman, Saulnier Mark G, Upender Velaparthi, Tai W. Wong, Mei-Li Wen, Kurt Zimmermann, Richard A. Westhouse, Adrian V. Lee, Ching Ping Ho
Publikováno v:
Cancer Research. 65:3781-3787
The insulin-like growth factor I receptor (IGF-IR) is a transmembrane tyrosine kinase that is essential to growth and development and also thought to provide a survival signal for the maintenance of the transformed phenotype. There has been increasin
Autor:
Thomas J. Altstadt, William C. Rose, Byron H. Long, Henry Wong, Mark D. Wittman, Mu-Jen Wu, Craig R. Fairchild, Kathy A. Johnston, Jerzy Golik, Dolatrai M. Vyas, John F. Kadow, Francis Y. Lee
Publikováno v:
Journal of Medicinal Chemistry. 44:4577-4583
The preparation of C-7 paclitaxel ethers is described. Various substituted ethers were prepared via activation of the corresponding methylthiomethyl ether followed by alcohol addition. Variation of the C-7 ether group as well the 3' side chain positi
Autor:
Kathy A. Johnston, Mark D. Wittman, Dolatrai M. Vyas, Craig Fairchild, Francis L. Lee, John F. Kadow, William C. Rose, Byron H. Long
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:811-814
The syntheses and antitumor activity of three paclitaxel-chlorambucil hybrids are presented. Hybrid 3 showed significant in vivo efficacy.