Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Mustapha Haddach"'
Autor:
William G. Rice, Kenna Anderes, David Ryckman, Ross D. Hannan, Megan J. Bywater, Elaine Sanij, Jaclyn E. Quin, Nicole Streiner, Adam Siddiqui-Jain, Michael K. Schwaebe, Mustapha Haddach, Mayuko Omori, Chris Proffitt, Sean E. O'Brien, Caroline B. Ho, Josh Bliesath, Amy Lin, Denis Drygin
Supplementary Materials from Targeting RNA Polymerase I with an Oral Small Molecule CX-5461 Inhibits Ribosomal RNA Synthesis and Solid Tumor Growth
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c0b64b9899bae18205e730a978712b0
https://doi.org/10.1158/0008-5472.22387916.v1
https://doi.org/10.1158/0008-5472.22387916.v1
Publikováno v:
Journal of Medicinal Chemistry. 55:8199-8208
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1a5ce6f3cf2bcfea42abfc1b255d6866
https://doi.org/10.1021/jm3009234
https://doi.org/10.1021/jm3009234
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:
Fabrice Pierre, Collin F. Regan, David M. Ryckman, Mustapha Haddach, Michael K. Schwaebe, Michael E. Jung
Publikováno v:
Synlett. 23:443-447
This paper reports the synthesis of various 5-halopyrimidine-4-carboxylic acid esters via the Minisci homolytic alkoxycarbonylation of 5-halopyrimidines. The reaction was found to be highly regioselective, allowing the one-step synthesis of useful am
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d6cd84a716460538e0a784b185ca3102
https://doi.org/10.1055/s-0031-1290136
https://doi.org/10.1055/s-0031-1290136
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:
Denis Drygin, Marie-Claire Chevrel, Anne‐Sophie Nedellec, Collin F. Regan, Diwata Macalino, Mustapha Haddach, Sean O'Brien, Adam Siddiqui-Jain, Kenna Anderes, Fabrice Pierre, Eric Stefan, Nicole Streiner, David M. Ryckman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6687-6692
A novel class of pan-Pim kinase inhibitors was designed by modifying the CK2 inhibitor CX-4945. Introduction of a triazole or secondary amide functionality on the C-7 position and 2'-halogenoanilines on C-5 resulted in potent inhibitors of the Pim-1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a38017ad454d36e6736d1c2acfc4a8d
https://doi.org/10.1016/j.bmcl.2011.09.059
https://doi.org/10.1016/j.bmcl.2011.09.059
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:
Johnny Y. Nagasawa, Michael K. Schwaebe, Fabrice Pierre, Mustapha Haddach, Anne Vialettes, David M. Ryckman
Publikováno v:
Tetrahedron Letters. 52:1096-1100
Quinolone esters are readily converted into the corresponding amides using aluminum chloride at room temperature in excellent yields and purities. The method is both general and scalable to multi-kilogram quantities.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c01e22faf3b70c36f997b52049fe13d1
https://doi.org/10.1016/j.tetlet.2010.12.108
https://doi.org/10.1016/j.tetlet.2010.12.108
Autor:
Charles Q. Huang, James R. McCarthy, Paul D. Crowe, Raymond S. Gross, John Saunders, Dimitri E. Grigoriadis, Jodene Nelson, Richard Lowe, Brian Dyck, John P. Williams, Dragan Marinkovic, Sam R. J. Hoare, Tim Coon, Robert W. Sullivan, Mustapha Haddach, Said Zamani-Kord, Manisha Moorjani, Zhiqiang Guo, Jane Han Bu, Takung Chen
Publikováno v:
Journal of Medicinal Chemistry. 48:5780-5793
Antagonists of the corticotropin-releasing factor (CRF) neuropeptide should prove to be effective in treating stress and anxiety-related disorders. In an effort to identify antagonists with improved physicochemical properties, new tricyclic CRF(1) an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ed6584cab9355c213297346348adfa0
https://doi.org/10.1021/jm049085v
https://doi.org/10.1021/jm049085v
Autor:
Said Zamani-Kord, Brian Dyck, Zhiqiang Guo, Robert W. Sullivan, Zhiyong Luo, Raymond S. Gross, Manisha Moorjani, Bin-Feng Li, Mustapha Haddach, John E. Tellew, Mehrak Kiankarimi, Marion Lanier, John P. Williams, James R. McCarthy, Dimitri Grigoriadis, Ta Kung Chen, Paul D. Crowe, John Saunders, Xiaohu Zhang, Jonathan Grey
Publikováno v:
Journal of Medicinal Chemistry. 48:5104-5107
The synthesis and SAR studies of tricyclic imidazo[4,5-b]pyridin-2-ones as human corticotropin-releasing factor receptor (CRF(1)) antagonists are discussed herein. Compound 16g was identified as a functional antagonist that inhibited CRF-stimulated c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::815355c45c4d5367cde1ab00c4dece95
https://doi.org/10.1021/jm050384+
https://doi.org/10.1021/jm050384+