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APTO-253 Stabilizes G-quadruplex DNA, Inhibits MYC Expression, and Induces DNA Damage in Acute Myeloid Leukemia Cells.

Local A, Zhang H, Benbatoul KD, Folger P, Sheng X, Tsai CY, Howell SB, Rice WG.

Mol Cancer Ther. 2018 Jun;17(6):1177-1186. doi: 10.1158/1535-7163.MCT-17-1209. Epub 2018 Apr 6.


APTO-253 Is a New Addition to the Repertoire of Drugs that Can Exploit DNA BRCA1/2 Deficiency.

Tsai CY, Sun S, Zhang H, Local A, Su Y, Gross LA, Rice WG, Howell SB.

Mol Cancer Ther. 2018 Jun;17(6):1167-1176. doi: 10.1158/1535-7163.MCT-17-0834. Epub 2018 Apr 6.


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.


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.


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.


The RNA polymerase I transcription machinery: an emerging target for the treatment of cancer.

Drygin D, Rice WG, Grummt I.

Annu Rev Pharmacol Toxicol. 2010;50:131-56. doi: 10.1146/annurev.pharmtox.010909.105844. Review.


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.


In vivo antiviral activity of novel human immunodeficiency virus type 1 nucleocapsid p7 zinc finger inhibitors in a transgenic murine model.

Schito ML, Goel A, Song Y, Inman JK, Fattah RJ, Rice WG, Turpin JA, Sher A, Appella E.

AIDS Res Hum Retroviruses. 2003 Feb;19(2):91-101.


Synthesis and biological properties of amino acid amide ligand-based pyridinioalkanoyl thioesters as anti-HIV agents.

Song Y, Goel A, Basrur V, Roberts PE, Mikovits JA, Inman JK, Turpin JA, Rice WG, Appella E.

Bioorg Med Chem. 2002 May;10(5):1263-73.


Benzamide-based thiolcarbamates: a new class of HIV-1 NCp7 inhibitors.

Goel A, Mazur SJ, Fattah RJ, Hartman TL, Turpin JA, Huang M, Rice WG, Appella E, Inman JK.

Bioorg Med Chem Lett. 2002 Mar 11;12(5):767-70.


The secondary amine/nitric oxide complex ion R(2)N[N(O)NO](-) as nucleophile and leaving group in S9N)Ar reactions.

Saavedra JE, Srinivasan A, Bonifant CL, Chu J, Shanklin AP, Flippen-Anderson JL, Rice WG, Turpin JA, Davies KM, Keefer LK.

J Org Chem. 2001 May 4;66(9):3090-8.


Inactivation of HIV-1 nucleocapsid protein P7 by pyridinioalkanoyl thioesters. Characterization of reaction products and proposed mechanism of action.

Basrur V, Song Y, Mazur SJ, Higashimoto Y, Turpin JA, Rice WG, Inman JK, Appella E.

J Biol Chem. 2000 May 19;275(20):14890-7.


Inhibition of G-protein-coupled receptor function by disruption of transmembrane domain interactions.

Tarasova NI, Rice WG, Michejda CJ.

J Biol Chem. 1999 Dec 3;274(49):34911-5.


Thiazolothiazepine inhibitors of HIV-1 integrase.

Neamati N, Turpin JA, Winslow HE, Christensen JL, Williamson K, Orr A, Rice WG, Pommier Y, Garofalo A, Brizzi A, Campiani G, Fiorini I, Nacci V.

J Med Chem. 1999 Aug 26;42(17):3334-41.


Potential drugs against cervical cancer: zinc-ejecting inhibitors of the human papillomavirus type 16 E6 oncoprotein.

Beerheide W, Bernard HU, Tan YJ, Ganesan A, Rice WG, Ting AE.

J Natl Cancer Inst. 1999 Jul 21;91(14):1211-20.


Extension of the polyanionic cosalane pharmacophore as a strategy for increasing anti-HIV potency.

Cushman M, Insaf S, Paul G, Ruell JA, De Clercq E, Schols D, Pannecouque C, Witvrouw M, Schaeffer CA, Turpin JA, Williamson K, Rice WG.

J Med Chem. 1999 May 20;42(10):1767-77.


Chicoric acid analogues as HIV-1 integrase inhibitors.

Lin Z, Neamati N, Zhao H, Kiryu Y, Turpin JA, Aberham C, Strebel K, Kohn K, Witvrouw M, Pannecouque C, Debyser Z, De Clercq E, Rice WG, Pommier Y, Burke TR Jr.

J Med Chem. 1999 Apr 22;42(8):1401-14.


Synthesis and biological properties of novel pyridinioalkanoyl thiolesters (PATE) as anti-HIV-1 agents that target the viral nucleocapsid protein zinc fingers.

Turpin JA, Song Y, Inman JK, Huang M, Wallqvist A, Maynard A, Covell DG, Rice WG, Appella E.

J Med Chem. 1999 Jan 14;42(1):67-86.


Synthesis of a non-nucleoside reverse transcriptase inhibitor in the alkenyldiarylmethane (ADAM) series with optimized potency and therapeutic index.

Cushman M, Casimiro-Garcia A, Williamson K, Rice WG.

Bioorg Med Chem Lett. 1998 Jan 20;8(2):195-8.


Synthesis of a cosalane analog with an extended polyanionic pharmacophore conferring enhanced potency as an anti-HIV agent.

Cushman M, Insaf S, Ruell JA, Schaeffer CA, Rice WG.

Bioorg Med Chem Lett. 1998 Apr 7;8(7):833-6.


Reactivity of the HIV-1 nucleocapsid protein p7 zinc finger domains from the perspective of density-functional theory.

Maynard AT, Huang M, Rice WG, Covell DG.

Proc Natl Acad Sci U S A. 1998 Sep 29;95(20):11578-83.


Small molecule inhibitor of HIV-1 cell fusion blocks chemokine receptor-mediated function.

Howard OM, Korte T, Tarasova NI, Grimm M, Turpin JA, Rice WG, Michejda CJ, Blumenthal R, Oppenheim JJ.

J Leukoc Biol. 1998 Jul;64(1):6-13. Review.


Inhibition of in vitro and in vivo HIV replication by a distamycin analogue that interferes with chemokine receptor function: a candidate for chemotherapeutic and microbicidal application.

Howard OM, Oppenheim JJ, Hollingshead MG, Covey JM, Bigelow J, McCormack JJ, Buckheit RW Jr, Clanton DJ, Turpin JA, Rice WG.

J Med Chem. 1998 Jun 18;41(13):2184-93.


New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors.

Cushman M, Casimiro-Garcia A, Hejchman E, Ruell JA, Huang M, Schaeffer CA, Williamson K, Rice WG, Buckheit RW Jr.

J Med Chem. 1998 Jun 4;41(12):2076-89.


Efficacies of zinc-finger-active drugs against Giardia lamblia.

Nash T, Rice WG.

Antimicrob Agents Chemother. 1998 Jun;42(6):1488-92.


Anti-HIV agents that selectively target retroviral nucleocapsid protein zinc fingers without affecting cellular zinc finger proteins.

Huang M, Maynard A, Turpin JA, Graham L, Janini GM, Covell DG, Rice WG.

J Med Chem. 1998 Apr 23;41(9):1371-81.


Inhibition of acute-, latent-, and chronic-phase human immunodeficiency virus type 1 (HIV-1) replication by a bistriazoloacridone analog that selectively inhibits HIV-1 transcription.

Turpin JA, Buckheit RW Jr, Derse D, Hollingshead M, Williamson K, Palamone C, Osterling MC, Hill SA, Graham L, Schaeffer CA, Bu M, Huang M, Cholody WM, Michejda CJ, Rice WG.

Antimicrob Agents Chemother. 1998 Mar;42(3):487-94.


Zinc ejection as a new rationale for the use of cystamine and related disulfide-containing antiviral agents in the treatment of AIDS.

McDonnell NB, De Guzman RN, Rice WG, Turpin JA, Summers MF.

J Med Chem. 1997 Jun 20;40(13):1969-76.


Differential infection of CD34+ cell-derived dendritic cells and monocytes with lymphocyte-tropic and monocyte-tropic HIV-1 strains.

Warren MK, Rose WL, Cone JL, Rice WG, Turpin JA.

J Immunol. 1997 May 15;158(10):5035-42.


A new class of anti-HIV-1 agents targeted toward the nucleocapsid protein NCp7: the 2,2'-dithiobisbenzamides.

Domagala JM, Bader JP, Gogliotti RD, Sanchez JP, Stier MA, Song Y, Prasad JV, Tummino PJ, Scholten J, Harvey P, Holler T, Gracheck S, Hupe D, Rice WG, Schultz R.

Bioorg Med Chem. 1997 Mar;5(3):569-79.


Azodicarbonamide inhibits HIV-1 replication by targeting the nucleocapsid protein.

Rice WG, Turpin JA, Huang M, Clanton D, Buckheit RW Jr, Covell DG, Wallqvist A, McDonnell NB, DeGuzman RN, Summers MF, Zalkow L, Bader JP, Haugwitz RD, Sausville EA.

Nat Med. 1997 Mar;3(3):341-5.


Inhibition of multiple phases of human immunodeficiency virus type 1 replication by a dithiane compound that attacks the conserved zinc fingers of retroviral nucleocapsid proteins.

Rice WG, Baker DC, Schaeffer CA, Graham L, Bu M, Terpening S, Clanton D, Schultz R, Bader JP, Buckheit RW Jr, Field L, Singh PK, Turpin JA.

Antimicrob Agents Chemother. 1997 Feb;41(2):419-26.


Virus-encoded Zinc Fingers as Targets for Antiviral Chemotherapy.

Rice WG, Turpin JA.

Rev Med Virol. 1996 Dec;6(4):187-199. No abstract available.


Inhibition of human immunodeficiency virus replication by the sulfonated stilbene dye resobene.

Halliday SM, Lackman-Smith C, Bader JP, Rice WG, Clanton DJ, Zalkow LH, Buckheit RW Jr.

Antiviral Res. 1996 Dec;33(1):41-53.


Evaluation of selected chemotypes in coupled cellular and molecular target-based screens identifies novel HIV-1 zinc finger inhibitors.

Rice WG, Turpin JA, Schaeffer CA, Graham L, Clanton D, Buckheit RW Jr, Zaharevitz D, Summers MF, Wallqvist A, Covell DG.

J Med Chem. 1996 Sep 13;39(19):3606-16.


Inhibitors of human immunodeficiency virus type 1 zinc fingers prevent normal processing of gag precursors and result in the release of noninfectious virus particles.

Turpin JA, Terpening SJ, Schaeffer CA, Yu G, Glover CJ, Felsted RL, Sausville EA, Rice WG.

J Virol. 1996 Sep;70(9):6180-9.


Synthesis and biological evaluation of certain alkenyldiarylmethanes as anti-HIV-1 agents which act as non-nucleoside reverse transcriptase inhibitors.

Cushman M, Golebiewski WM, Graham L, Turpin JA, Rice WG, Fliakas-Boltz V, Buckheit RW Jr.

J Med Chem. 1996 Aug 2;39(16):3217-27.


Antiretroviral agents as inhibitors of both human immunodeficiency virus type 1 integrase and protease.

Mazumder A, Wang S, Neamati N, Nicklaus M, Sunder S, Chen J, Milne GW, Rice WG, Burke TR Jr, Pommier Y.

J Med Chem. 1996 Jun 21;39(13):2472-81.


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