Zobrazeno 1 - 10
of 23
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8f3160afd93213ef74a7ceb68cacac8b
https://doi.org/10.1016/j.bmcl.2011.11.087
https://doi.org/10.1016/j.bmcl.2011.11.087
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8047df7df0af652af52401571f4b18f3
https://doi.org/10.1007/s11010-011-0956-5
https://doi.org/10.1007/s11010-011-0956-5
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::269ff3db6ed32096f1a6a4ca7c08854c
https://doi.org/10.1016/j.tetlet.2008.05.005
https://doi.org/10.1016/j.tetlet.2008.05.005
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8fd978c4cbd83bf7095f40407e6e696b
https://doi.org/10.1016/j.bmcl.2008.05.084
https://doi.org/10.1016/j.bmcl.2008.05.084
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.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c7fd044ba3041bdae84613f10c01e2c8
https://doi.org/10.1007/s007830050057
https://doi.org/10.1007/s007830050057
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f439bce1d155b695409817b81d1259ae
https://doi.org/10.1016/s0040-4039(97)10505-6
https://doi.org/10.1016/s0040-4039(97)10505-6
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::02b23c94c8d9e34084b63fa53beb40dc
https://doi.org/10.1016/s0040-4039(97)10310-0
https://doi.org/10.1016/s0040-4039(97)10310-0
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1dbc121864d837264b8a980c6fc2425b
https://doi.org/10.2478/tumor-2013-0003
https://doi.org/10.2478/tumor-2013-0003
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::31b3836bca12986c54995b11df46be4a
https://doi.org/10.1158/1538-7445.am2016-4780
https://doi.org/10.1158/1538-7445.am2016-4780
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::381f31afdb18ac8eca61f6768c660619
https://pubmed.ncbi.nlm.nih.gov/21174434
https://pubmed.ncbi.nlm.nih.gov/21174434