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Items: 24


Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization.

Siddiqui-Jain A, Hoj JP, Cescon DW, Hansen MD.

Bioorg Med Chem Lett. 2018 Mar 1;28(5):934-941. doi: 10.1016/j.bmcl.2018.01.053. Epub 2018 Feb 9.


Combined venetoclax and alvocidib in acute myeloid leukemia.

Bogenberger J, Whatcott C, Hansen N, Delman D, Shi CX, Kim W, Haws H, Soh K, Lee YS, Peterson P, Siddiqui-Jain A, Weitman S, Stewart K, Bearss D, Mesa R, Warner S, Tibes R.

Oncotarget. 2017 Nov 3;8(63):107206-107222. doi: 10.18632/oncotarget.22284. eCollection 2017 Dec 5.


Pyridine-pyrimidine amides that prevent HGF-induced epithelial scattering by two distinct mechanisms.

Siddiqui-Jain A, Hoj JP, Hargiss JB, Hoj TH, Payne CJ, Ritchie CA, Herron SR, Quinn C, Schuler JT, Hansen MDH.

Bioorg Med Chem Lett. 2017 Sep 1;27(17):3992-4000. doi: 10.1016/j.bmcl.2017.07.063. Epub 2017 Jul 25.


DNA structure: Visualizing the quadruplex.

Siddiqui-Jain A, Hurley LH.

Nat Chem. 2013 Mar;5(3):153-5. doi: 10.1038/nchem.1587. No abstract available.


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.


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.


Combined inhibition of EGFR and CK2 augments the attenuation of PI3K-Akt-mTOR signaling and the killing of cancer cells.

Bliesath J, Huser N, Omori M, Bunag D, Proffitt C, Streiner N, Ho C, Siddiqui-Jain A, O'Brien SE, Lim JK, Ryckman DM, Anderes K, Rice WG, Drygin D.

Cancer Lett. 2012 Sep 1;322(1):113-8. doi: 10.1016/j.canlet.2012.02.032. Epub 2012 Mar 2.


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.


CK2 inhibitor CX-4945 suppresses DNA repair response triggered by DNA-targeted anticancer drugs and augments efficacy: mechanistic rationale for drug combination therapy.

Siddiqui-Jain A, Bliesath J, Macalino D, Omori M, Huser N, Streiner N, Ho CB, Anderes K, Proffitt C, O'Brien SE, Lim JK, Von Hoff DD, Ryckman DM, Rice WG, Drygin D.

Mol Cancer Ther. 2012 Apr;11(4):994-1005. doi: 10.1158/1535-7163.MCT-11-0613. Epub 2012 Jan 20.


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.


Protein kinase CK2 modulates IL-6 expression in inflammatory breast cancer.

Drygin D, Ho CB, Omori M, Bliesath J, Proffitt C, Rice R, Siddiqui-Jain A, O'Brien S, Padgett C, Lim JK, Anderes K, Rice WG, Ryckman D.

Biochem Biophys Res Commun. 2011 Nov 11;415(1):163-7. doi: 10.1016/j.bbrc.2011.10.046. Epub 2011 Oct 18.


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.


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.


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.


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.


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.


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.


CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy.

Siddiqui-Jain A, Drygin D, Streiner N, Chua P, Pierre F, O'Brien SE, Bliesath J, Omori M, Huser N, Ho C, Proffitt C, Schwaebe MK, Ryckman DM, Rice WG, Anderes K.

Cancer Res. 2010 Dec 15;70(24):10288-98. doi: 10.1158/0008-5472.CAN-10-1893.


Anticancer activity of CX-3543: a direct inhibitor of rRNA biogenesis.

Drygin D, Siddiqui-Jain A, O'Brien S, Schwaebe M, Lin A, Bliesath J, Ho CB, Proffitt C, Trent K, Whitten JP, Lim JK, Von Hoff D, Anderes K, Rice WG.

Cancer Res. 2009 Oct 1;69(19):7653-61. doi: 10.1158/0008-5472.CAN-09-1304. Epub 2009 Sep 8.


Drug targeting of the c-MYC promoter to repress gene expression via a G-quadruplex silencer element.

Hurley LH, Von Hoff DD, Siddiqui-Jain A, Yang D.

Semin Oncol. 2006 Aug;33(4):498-512. Review.


Conformationally restricted analogues of psorospermin: design, synthesis, and bioactivity of natural-product-related bisfuranoxanthones.

Heald RA, Dexheimer TS, Vankayalapati H, Siddiqui-Jain A, Szabo LZ, Gleason-Guzman MC, Hurley LH.

J Med Chem. 2005 Apr 21;48(8):2993-3004.


Design and synthesis of an expanded porphyrin that has selectivity for the c-MYC G-quadruplex structure.

Seenisamy J, Bashyam S, Gokhale V, Vankayalapati H, Sun D, Siddiqui-Jain A, Streiner N, Shin-Ya K, White E, Wilson WD, Hurley LH.

J Am Chem Soc. 2005 Mar 9;127(9):2944-59.


The dynamic character of the G-quadruplex element in the c-MYC promoter and modification by TMPyP4.

Seenisamy J, Rezler EM, Powell TJ, Tye D, Gokhale V, Joshi CS, Siddiqui-Jain A, Hurley LH.

J Am Chem Soc. 2004 Jul 21;126(28):8702-9.


Direct evidence for a G-quadruplex in a promoter region and its targeting with a small molecule to repress c-MYC transcription.

Siddiqui-Jain A, Grand CL, Bearss DJ, Hurley LH.

Proc Natl Acad Sci U S A. 2002 Sep 3;99(18):11593-8. Epub 2002 Aug 23.

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