Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Peter C. Chua"'
Autor:
Denis Drygin, Jerome Michaux, Fabrice Pierre, Diwata Macalino, Mustapha Haddach, Cosmin Borsan, David M. Ryckman, Collin F. Regan, Sean O'Brien, Pauline Kerdoncuff, Eric Stefan, Adam Siddiqui-Jain, Peter C. Chua, Michael K. Schwaebe, William G. Rice
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:45-48
Protein kinase CK2 is a potential drug target for many diseases including cancer and inflammation disorders. The crystal structure of clinical candidate CX-4945 1 with CK2 revealed an indirect interaction with the protein through hydrogen bonding bet
Autor:
Chris Proffitt, Johnny Y. Nagasawa, Levan Darjania, Eric Stefan, Ryan Stansfield, Sean O'Brien, Nicole Streiner, Jeffrey P. Whitten, Joshua R. Bliesath, Peter C. Chua, Caroline B. Ho, Pauline Bourbon, William G. Rice, Fabrice Pierre, Adam Siddiqui-Jain, Ta Kung Chen, Kenna Anderes, Anne Vialettes, Mustapha Haddach, David M. Ryckman, Michael K. Schwaebe, Denis Drygin, Jerome Michaux, May Omori
Publikováno v:
Molecular and Cellular Biochemistry. 356:37-43
In this article we describe the preclinical characterization of 5-(3-chlorophenylamino) benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first orally available small molecule inhibitor of protein CK2 in clinical trials for cancer. CX-4945
Autor:
Peter C. Chua, Michael K. Schwaebe, Johnny Y. Nagasawa, Anne Vialettes, Jeffrey P. Whitten, Fabrice Pierre
Publikováno v:
Tetrahedron Letters. 49:4437-4442
A novel and efficient synthesis of 5-oxo-6-carboxy-naphthyridines is reported in this Letter along with a discussion of scope and limitations. Activated 3-nicotinic acids readily acylate the magnesium anion of 2-(benzothiazol-2-yl) or 2-(benzimidazol
Autor:
Peter C. Chua, Yiwei Li, Jun Liang, Johnny Y. Nagasawa, Raymond E. Jones, Stanley F. Barnett, Lida R. Tehrani, Ronald G. Robinson, Deborah Defeo-Jones, Tony Siu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4191-4194
This letter details the attenuation of hERG in a class of Akt inhibitors through heteroatom insertions into aromatic rings. The development of a cell-active dual Akt 1 and 2 inhibitors devoid of hERG activity is discussed using structure-activity rel
Autor:
Peter C. Chua, André B. Charette
Publikováno v:
Molecules Online. 2:63-75
The enantioselective syntheses of naphthyl-substituted-N-tosylphenylglycines are described. These unnatural amino acids were tested as ligands for the chiral oxazaborolidine catalyzed Diels-Alder reaction between cyclopentadiene and 2-bromoacrolein.
Autor:
André B. Charette, Peter C. Chua
Publikováno v:
Tetrahedron Letters. 39:245-248
Secondary and tertiary amides were treated with trifluoromethanesulfonic (triflic) anhydride in the presence of pyridine at low temperatures to generate imino and iminium triflates. Subsequent treatment with hydrogen sulfide immediately gave rise to
Autor:
André B. Charette, Peter C. Chua
Publikováno v:
Tetrahedron Letters. 38:8499-8502
Secondary and tertiary amides were treated with trifluoromethanesulfonic (triflic) anhydride in the presence of pyridine at low temperatures to generate imino and iminium triflates. Successive treatment with 2,2-bishydroxymethyl-1-propanol in the pyr
Autor:
Peter C. Chua, Jordan Cran, Karlo Kordic, Jason S. Tan, Geoffrey C. Winters, James W. Evans, Andrew I. Minchinton, Alastair H. Kyle, Jerome Lozada, Kirstin E. Lindquist
Publikováno v:
Tumor Microenvironment and Therapy. 1
Tumour hypoxia presents a barrier to conventional chemotherapy and radiation therapy. To combat hypoxic cells a number of hypoxia modifying treatments are currently in development. In this study we assessed the potential for inhibiting DNA double str
Autor:
Pratik S. Multani, Jennifer W. Oliver, Jerry Cao, Gary G. Li, Ralph Lin, Michael D. Johnson, Leenus Martin, Peter C. Chua, R. Patel, Robert A. Wild, Colin Walsh
Publikováno v:
Cancer Research. 76:4780-4780
RXDX-107 is a dodecanol alkyl ester of bendamustine, which is then encapsulated in human serum albumin (HSA) to form nanoparticles. Bendamustine is an alkylating agent that induces interstrand DNA crosslinks (ICLs) and causes cell death via several p
Autor:
Jeffrey P. Whitten, Katy Trent, Caroline B. Ho, Kenna Anderes, Anne Vialettes, May Omori, Adam Siddiqui-Jain, Sean O'Brien, Johnny Y. Nagasawa, Michael K. Schwaebe, Eric Stefan, William G. Rice, Pauline Bourbon, Peter C. Chua, Ta Kung Chen, Chris Proffitt, Fabrice Pierre, Denis Drygin, Mustapha Haddach, Jerome Michaux, Nicole Streiner, Levan Darjania, David M. Ryckman, Ryan Stansfield, Josh Bliesath
Publikováno v:
Journal of medicinal chemistry. 54(2)
Herein we chronicle the discovery of CX-4945 (25n), a first-in-class, orally bioavailable ATP-competitive inhibitor of protein kinase CK2 in clinical trials for cancer. CK2 has long been considered a prime cancer drug target because of the roles of d