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18 results

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Page 1
Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties.
Pierre F, O'Brien SE, Haddach M, Bourbon P, Schwaebe MK, Stefan E, Darjania L, Stansfield R, Ho C, Siddiqui-Jain A, Streiner N, Rice WG, Anderes K, Ryckman DM. Pierre F, et al. Among authors: haddach m. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1687-91. doi: 10.1016/j.bmcl.2011.01.091. Epub 2011 Jan 26. Bioorg Med Chem Lett. 2011. PMID: 21316963
Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.
Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E, Vialettes A, Whitten JP, Chen TK, Darjania L, Stansfield R, Anderes K, Bliesath J, Drygin D, Ho C, Omori M, Proffitt C, Streiner N, Trent K, Rice WG, Ryckman DM. Pierre F, et al. Among authors: haddach m. J Med Chem. 2011 Jan 27;54(2):635-54. doi: 10.1021/jm101251q. Epub 2010 Dec 21. J Med Chem. 2011. PMID: 21174434
Pre-clinical characterization of CX-4945, a potent and selective small molecule inhibitor of CK2 for the treatment of cancer.
Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E, Vialettes A, Whitten JP, Chen TK, Darjania L, Stansfield R, Bliesath J, Drygin D, Ho C, Omori M, Proffitt C, Streiner N, Rice WG, Ryckman DM, Anderes K. Pierre F, et al. Among authors: haddach m. Mol Cell Biochem. 2011 Oct;356(1-2):37-43. doi: 10.1007/s11010-011-0956-5. Epub 2011 Jul 14. Mol Cell Biochem. 2011. PMID: 21755459
7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity.
Pierre F, Stefan E, Nédellec AS, Chevrel MC, Regan CF, Siddiqui-Jain A, Macalino D, Streiner N, Drygin D, Haddach M, O'Brien SE, Anderes K, Ryckman DM. Pierre F, et al. Among authors: haddach m. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6687-92. doi: 10.1016/j.bmcl.2011.09.059. Epub 2011 Sep 22. Bioorg Med Chem Lett. 2011. PMID: 21982499
Synthesis and SAR of inhibitors of protein kinase CK2: novel tricyclic quinoline analogs.
Haddach M, Pierre F, Regan CF, Borsan C, Michaux J, Stefan E, Kerdoncuff P, Schwaebe MK, Chua PC, Siddiqui-Jain A, Macalino D, Drygin D, O'Brien SE, Rice WG, Ryckman DM. Haddach M, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):45-8. doi: 10.1016/j.bmcl.2011.11.087. Epub 2011 Nov 30. Bioorg Med Chem Lett. 2012. PMID: 22169261
Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth.
Drygin D, Lin A, Bliesath J, Ho CB, O'Brien SE, Proffitt C, Omori M, Haddach M, Schwaebe MK, Siddiqui-Jain A, Streiner N, Quin JE, Sanij E, Bywater MJ, Hannan RD, Ryckman D, Anderes K, Rice WG. Drygin D, et al. Among authors: haddach m. Cancer Res. 2011 Feb 15;71(4):1418-30. doi: 10.1158/0008-5472.CAN-10-1728. Epub 2010 Dec 15. Cancer Res. 2011. PMID: 21159662
Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer.
Battistutta R, Cozza G, Pierre F, Papinutto E, Lolli G, Sarno S, O'Brien SE, Siddiqui-Jain A, Haddach M, Anderes K, Ryckman DM, Meggio F, Pinna LA. Battistutta R, et al. Among authors: haddach m. Biochemistry. 2011 Oct 4;50(39):8478-88. doi: 10.1021/bi2008382. Epub 2011 Sep 7. Biochemistry. 2011. PMID: 21870818
Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.
Haddach M, Michaux J, Schwaebe MK, Pierre F, O'Brien SE, Borsan C, Tran J, Raffaele N, Ravula S, Drygin D, Siddiqui-Jain A, Darjania L, Stansfield R, Proffitt C, Macalino D, Streiner N, Bliesath J, Omori M, Whitten JP, Anderes K, Rice WG, Ryckman DM. Haddach M, et al. ACS Med Chem Lett. 2011 Dec 27;3(2):135-9. doi: 10.1021/ml200259q. eCollection 2012 Feb 9. ACS Med Chem Lett. 2011. PMID: 24900437 Free PMC article.
18 results