Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Jerome Michaux"'
Publikováno v:
Tetrahedron Letters
Tetrahedron Letters, Elsevier, 2014, 55 (17), pp.2849-2852. ⟨10.1016/j.tetlet.2014.03.081⟩
Tetrahedron Letters, Elsevier, 2014, 55 (17), pp.2849-2852. ⟨10.1016/j.tetlet.2014.03.081⟩
Highly strained pentacyclic bis-lactones can be obtained by an unusual Co(I) catalyzed [2+2+2] cycloaddition of an yne–ene–yne diester substrate. These bis-lactones can be further transformed into tetraaryl N-hydroxyphthalimides which are potenti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e34fc7d3381ac96e498e02bd122361b5
https://doi.org/10.1016/j.tetlet.2014.03.081
https://doi.org/10.1016/j.tetlet.2014.03.081
Autor:
Jeffrey P. Whitten, Ryan Stansfield, Chris Proffitt, Adam Siddiqui-Jain, Johnny Y. Nagasawa, Josh Bliesath, Pauline Kerdoncuff, Kenna Anderes, David M. Ryckman, Nanni Huser, May Omori, Levan Darjania, William G. Rice, Mustapha Haddach, Denis Drygin, Jerome Michaux, Michael K. Schwaebe, Fabrice Pierre, Sean O'Brien
Publikováno v:
ACS Medicinal Chemistry Letters. 3:602-606
Accelerated proliferation of solid tumor and hematologic cancer cells is linked to accelerated transcription of rDNA by the RNA polymerase I (Pol I) enzyme to produce elevated levels of rRNA (rRNA). Indeed, upregulation of Pol I, frequently caused by
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::472fd5810e796ea42951640dfe4fa1ba
https://doi.org/10.1021/ml300110s
https://doi.org/10.1021/ml300110s
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
Publikováno v:
Tetrahedron Letters
Tetrahedron Letters, Elsevier, 2012, 53 (1), pp.48-50. ⟨10.1016/J.Tetlet.2011.10.114⟩
Tetrahedron Letters, Elsevier, 2012, 53 (1), pp.48-50. ⟨10.1016/J.Tetlet.2011.10.114⟩
The one pot, in situ ortho-metalation/silylation of unprotected o-phthalic acids using lithium tetramethylpiperidide (LiTMP) and chlorotrimethylsilane is described. This method gives a straightforward access to silylated phthalic anhydrides. These ca
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61fcc7070fefdd02b83988f3cd72844c
https://hal.archives-ouvertes.fr/hal-01654794
https://hal.archives-ouvertes.fr/hal-01654794
Autor:
Fabrice Pierre, Adam Siddiqui-Jain, Jeffrey P. Whitten, Ryan Stansfield, Levan Darjania, Cosmin Borsan, Sean O'Brien, Tran Joe, Chris Proffitt, May Omori, William G. Rice, Mustapha Haddach, Kenna Anderes, Nicholas B. Raffaele, Michael K. Schwaebe, Joshua R. Bliesath, Nicole Streiner, Suchitra Ravula, Diwata Macalino, Denis Drygin, Jerome Michaux, David M. Ryckman
Publikováno v:
ACS medicinal chemistry letters. 3(2)
Structure–activity relationship analysis in a series of 3-(5-((2-oxoindolin-3-ylidene)methyl)furan-2-yl)amides identified compound 13, a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity. Compound 13 exhibited in v
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df43fa65795ab6b23c07ba2ecc4b4594
https://pubmed.ncbi.nlm.nih.gov/24900437
https://pubmed.ncbi.nlm.nih.gov/24900437
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
Autor:
Michael K. Schwaebe, Denis Drygin, Cosmin Borsan, Jerome Michaux, Caroline B. Ho, Ryan Stansfield, Josh Bliesath, Pauline Kerdoncuff, William L. Rice, Fabrice Pierre, Mustapha Haddach, Kenna Anderes, May Omori, David M. Ryckman, Eric Stefan, Adam Siddiqui-Jain, Nicole Streiner, Jennifer Phung, Anne‐Sophie Nedellec, Diwata Macalino, Sean O'Brien
Publikováno v:
Molecular Cancer Therapeutics. 8:A246-A246
The PIM family of serine/threonine kinases are pro-proliferative kinases activated by multiple cytokines and growth factor signaling. The Pim kinases are unusual in that they are regulated primarily by transcription and not by membrane recruitment or
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b9a2d3c74d73f8697b7046fc262a85de
https://doi.org/10.1158/1535-7163.targ-09-a246
https://doi.org/10.1158/1535-7163.targ-09-a246
Autor:
Josh Bliesath, David M. Ryckman, Mike Schwaebe, Nicole Streiner, Anne Sophie Nedellec, Fabrice Pierre, William L. Rice, Kenna Anderes, Pauline Kerdoncuff, Sean O'Brien, Mustapha Haddach, Denis Drygin, May Omori, Jerome Michaux, Adam Siddiqui-Jain, Ryan Stansfield, Cosmin Borsan, Diwata Macalino, Caroline B. Ho, Eric Stefan, Jennifer Phung
Publikováno v:
Blood. 114:1726-1726
Abstract 1726 Poster Board I-752 The PIM family of serine/threonine kinases are pro-proliferative kinases activated by multiple cytokines and growth factor signaling. The Pim kinases are unusual in that they are regulated primarily by transcription a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bfad8fa2a69b38f35075f96fceea75a6
https://doi.org/10.1182/blood.v114.22.1726.1726
https://doi.org/10.1182/blood.v114.22.1726.1726
Autor:
Fabrice Pierre, Peter C. Chua, Sean E. O’Brien, Adam Siddiqui-Jain, Pauline Bourbon, Mustapha Haddach, Jerome Michaux, Johnny Nagasawa, Michael K. Schwaebe, Eric Stefan, Anne Vialettes, Jeffrey P. Whitten, Ta Kung Chen, Levan Darjania, Ryan Stansfield, Kenna Anderes, Josh Bliesath, Denis Drygin, Caroline Ho, May Omori
Publikováno v:
Journal of Medicinal Chemistry; Jan2011, Vol. 54 Issue 2, p635-654, 20p