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Items: 18

1.

Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy.

Drygin D, Haddach M, Pierre F, Ryckman DM.

J Med Chem. 2012 Oct 11;55(19):8199-208. doi: 10.1021/jm3009234. Epub 2012 Sep 4. No abstract available.

PMID:
22924342
2.

Inhibition of RNA polymerase I as a therapeutic strategy to promote cancer-specific activation of p53.

Bywater MJ, Poortinga G, Sanij E, Hein N, Peck A, Cullinane C, Wall M, Cluse L, Drygin D, Anderes K, Huser N, Proffitt C, Bliesath J, Haddach M, Schwaebe MK, Ryckman DM, Rice WG, Schmitt C, Lowe SW, Johnstone RW, Pearson RB, McArthur GA, Hannan RD.

Cancer Cell. 2012 Jul 10;22(1):51-65. doi: 10.1016/j.ccr.2012.05.019.

3.

Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics.

Haddach M, Schwaebe MK, Michaux J, Nagasawa J, O'Brien SE, Whitten JP, Pierre F, Kerdoncuff P, Darjania L, Stansfield R, Drygin D, Anderes K, Proffitt C, Bliesath J, Siddiqui-Jain A, Omori M, Huser N, Rice WG, Ryckman DM.

ACS Med Chem Lett. 2012 May 8;3(7):602-6. doi: 10.1021/ml300110s. eCollection 2012 Jul 12.

4.

Novel potent dual inhibitors of CK2 and Pim kinases with antiproliferative activity against cancer cells.

Pierre F, Regan CF, Chevrel MC, Siddiqui-Jain A, Macalino D, Streiner N, Drygin D, Haddach M, O'Brien SE, Rice WG, Ryckman DM.

Bioorg Med Chem Lett. 2012 May 1;22(9):3327-31. doi: 10.1016/j.bmcl.2012.02.099. Epub 2012 Mar 6.

PMID:
22460033
5.

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.

ACS Med Chem Lett. 2011 Dec 27;3(2):135-9. doi: 10.1021/ml200259q. eCollection 2012 Feb 9.

6.

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.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):45-8. doi: 10.1016/j.bmcl.2011.11.087. Epub 2011 Nov 30.

PMID:
22169261
7.

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, N├ędellec AS, Chevrel MC, Regan CF, Siddiqui-Jain A, Macalino D, Streiner N, Drygin D, Haddach M, O'Brien SE, Anderes K, Ryckman DM.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6687-92. doi: 10.1016/j.bmcl.2011.09.059. Epub 2011 Sep 22.

PMID:
21982499
8.

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.

Biochemistry. 2011 Oct 4;50(39):8478-88. doi: 10.1021/bi2008382. Epub 2011 Sep 7.

PMID:
21870818
9.

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.

Mol Cell Biochem. 2011 Oct;356(1-2):37-43. doi: 10.1007/s11010-011-0956-5. Epub 2011 Jul 14.

PMID:
21755459
10.

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.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1687-91. doi: 10.1016/j.bmcl.2011.01.091. Epub 2011 Jan 26.

PMID:
21316963
11.

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.

J Med Chem. 2011 Jan 27;54(2):635-54. doi: 10.1021/jm101251q. Epub 2010 Dec 21.

PMID:
21174434
12.

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.

Cancer Res. 2011 Feb 15;71(4):1418-30. doi: 10.1158/0008-5472.CAN-10-1728. Epub 2010 Dec 15.

13.

Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.

Gross RS, Guo Z, Dyck B, Coon T, Huang CQ, Lowe RF, Marinkovic D, Moorjani M, Nelson J, Zamani-Kord S, Grigoriadis DE, Hoare SR, Crowe PD, Bu JH, Haddach M, McCarthy J, Saunders J, Sullivan R, Chen T, Williams JP.

J Med Chem. 2005 Sep 8;48(18):5780-93.

PMID:
16134945
14.

Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.

Guo Z, Tellew JE, Gross RS, Dyck B, Grey J, Haddach M, Kiankarimi M, Lanier M, Li BF, Luo Z, McCarthy JR, Moorjani M, Saunders J, Sullivan R, Zhang X, Zamani-Kord S, Grigoriadis DE, Crowe PD, Chen TK, Williams JP.

J Med Chem. 2005 Aug 11;48(16):5104-7.

PMID:
16078829
15.

Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.

Dyck B, Grigoriadis DE, Gross RS, Guo Z, Haddach M, Marinkovic D, McCarthy JR, Moorjani M, Regan CF, Saunders J, Schwaebe MK, Szabo T, Williams JP, Zhang X, Bozigian H, Chen TK.

J Med Chem. 2005 Jun 16;48(12):4100-10.

PMID:
15943483
16.

Potent imidazole and triazole CB1 receptor antagonists related to SR141716.

Dyck B, Goodfellow VS, Phillips T, Grey J, Haddach M, Rowbottom M, Naeve GS, Brown B, Saunders J.

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1151-4.

PMID:
14980654
17.

Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists.

Huang CQ, Wilcoxen K, McCarthy JR, Haddach M, Webb TR, Gu J, Xie YF, Grigoriadis DE, Chen C.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3375-9.

PMID:
12951129
18.

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