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Items: 1 to 50 of 153

1.

Advances in the structural studies of antibiotic potentiators against Escherichia coli.

Blankson GA, Parhi AK, Kaul M, Pilch DS, LaVoie EJ.

Bioorg Med Chem. 2019 Aug 1;27(15):3254-3278. doi: 10.1016/j.bmc.2019.06.003. Epub 2019 Jun 4. No abstract available.

PMID:
31235265
2.

Structure-activity relationships of potentiators of the antibiotic activity of clarithromycin against Escherichia coli.

Blankson G, Parhi AK, Kaul M, Pilch DS, LaVoie EJ.

Eur J Med Chem. 2019 Sep 15;178:30-38. doi: 10.1016/j.ejmech.2019.05.075. Epub 2019 May 29.

PMID:
31173969
3.

Aryl and Arylalkyl Substituted 3-Hydroxypyridin-2(1H)-ones: Synthesis and Evaluation as Inhibitors of Influenza A Endonuclease.

Sagong HY, Bauman JD, Nogales A, Martínez-Sobrido L, Arnold E, LaVoie EJ.

ChemMedChem. 2019 Jun 18;14(12):1204-1223. doi: 10.1002/cmdc.201900084. Epub 2019 May 14.

PMID:
30983160
4.

β-Lactam Antibiotics with a High Affinity for PBP2 Act Synergistically with the FtsZ-Targeting Agent TXA707 against Methicillin-Resistant Staphylococcus aureus.

Ferrer-González E, Kaul M, Parhi AK, LaVoie EJ, Pilch DS.

Antimicrob Agents Chemother. 2017 Aug 24;61(9). pii: e00863-17. doi: 10.1128/AAC.00863-17. Print 2017 Sep.

5.

Structural Flexibility of an Inhibitor Overcomes Drug Resistance Mutations in Staphylococcus aureus FtsZ.

Fujita J, Maeda Y, Mizohata E, Inoue T, Kaul M, Parhi AK, LaVoie EJ, Pilch DS, Matsumura H.

ACS Chem Biol. 2017 Jul 21;12(7):1947-1955. doi: 10.1021/acschembio.7b00323. Epub 2017 Jun 16.

6.

Combining the FtsZ-Targeting Prodrug TXA709 and the Cephalosporin Cefdinir Confers Synergy and Reduces the Frequency of Resistance in Methicillin-Resistant Staphylococcus aureus.

Kaul M, Mark L, Parhi AK, LaVoie EJ, Pilch DS.

Antimicrob Agents Chemother. 2016 Jun 20;60(7):4290-6. doi: 10.1128/AAC.00613-16. Print 2016 Jul.

7.

TXA709, an FtsZ-Targeting Benzamide Prodrug with Improved Pharmacokinetics and Enhanced In Vivo Efficacy against Methicillin-Resistant Staphylococcus aureus.

Kaul M, Mark L, Zhang Y, Parhi AK, Lyu YL, Pawlak J, Saravolatz S, Saravolatz LD, Weinstein MP, LaVoie EJ, Pilch DS.

Antimicrob Agents Chemother. 2015 Aug;59(8):4845-55. doi: 10.1128/AAC.00708-15. Epub 2015 Jun 1.

8.

TXA497 as a topical antibacterial agent: comparative antistaphylococcal, skin deposition, and skin permeation studies with mupirocin.

Dorrani M, Kaul M, Parhi A, LaVoie EJ, Pilch DS, Michniak-Kohn B.

Int J Pharm. 2014 Dec 10;476(1-2):199-204. doi: 10.1016/j.ijpharm.2014.09.033. Epub 2014 Sep 26.

PMID:
25263100
9.

Phenyl substituted 4-hydroxypyridazin-3(2H)-ones and 5-hydroxypyrimidin-4(3H)-ones: inhibitors of influenza A endonuclease.

Sagong HY, Bauman JD, Patel D, Das K, Arnold E, LaVoie EJ.

J Med Chem. 2014 Oct 9;57(19):8086-98. doi: 10.1021/jm500958x. Epub 2014 Sep 29.

10.

3-Hydroxyquinolin-2(1H)-ones As Inhibitors of Influenza A Endonuclease.

Sagong HY, Parhi A, Bauman JD, Patel D, Vijayan RS, Das K, Arnold E, LaVoie EJ.

ACS Med Chem Lett. 2013 May 7;4(6):547-50. doi: 10.1021/ml4001112. eCollection 2013 Jun 13.

11.

Inhibition of RND-type efflux pumps confers the FtsZ-directed prodrug TXY436 with activity against Gram-negative bacteria.

Kaul M, Zhang Y, Parhi AK, Lavoie EJ, Pilch DS.

Biochem Pharmacol. 2014 Jun 1;89(3):321-8. doi: 10.1016/j.bcp.2014.03.002. Epub 2014 Mar 14.

PMID:
24637241
12.

Pharmacokinetics and in vivo antistaphylococcal efficacy of TXY541, a 1-methylpiperidine-4-carboxamide prodrug of PC190723.

Kaul M, Mark L, Zhang Y, Parhi AK, LaVoie EJ, Pilch DS.

Biochem Pharmacol. 2013 Dec 15;86(12):1699-707. doi: 10.1016/j.bcp.2013.10.010. Epub 2013 Oct 20.

PMID:
24148278
13.

Macrocyclic pyridyl polyoxazoles: structure-activity studies of the aminoalkyl side-chain on G-quadruplex stabilization and cytotoxic activity.

Blankson G, Rzuczek SG, Bishop C, Pilch DS, Liu A, Liu L, Lavoie EJ, Rice JE.

Molecules. 2013 Sep 26;18(10):11938-63. doi: 10.3390/molecules181011938.

14.

Phenyl substituted 3-hydroxypyridin-2(1H)-ones: inhibitors of influenza A endonuclease.

Parhi AK, Xiang A, Bauman JD, Patel D, Vijayan RS, Das K, Arnold E, Lavoie EJ.

Bioorg Med Chem. 2013 Nov 1;21(21):6435-46. doi: 10.1016/j.bmc.2013.08.053. Epub 2013 Sep 4.

PMID:
24055080
15.

An FtsZ-targeting prodrug with oral antistaphylococcal efficacy in vivo.

Kaul M, Mark L, Zhang Y, Parhi AK, Lavoie EJ, Pilch DS.

Antimicrob Agents Chemother. 2013 Dec;57(12):5860-9. doi: 10.1128/AAC.01016-13. Epub 2013 Sep 16.

16.

Crystallographic fragment screening and structure-based optimization yields a new class of influenza endonuclease inhibitors.

Bauman JD, Patel D, Baker SF, Vijayan RS, Xiang A, Parhi AK, Martínez-Sobrido L, LaVoie EJ, Das K, Arnold E.

ACS Chem Biol. 2013 Nov 15;8(11):2501-8. doi: 10.1021/cb400400j. Epub 2013 Sep 13.

17.

Antibacterial activity of quinoxalines, quinazolines, and 1,5-naphthyridines.

Parhi AK, Zhang Y, Saionz KW, Pradhan P, Kaul M, Trivedi K, Pilch DS, LaVoie EJ.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4968-74. doi: 10.1016/j.bmcl.2013.06.048. Epub 2013 Jun 26.

18.

Enterococcal and streptococcal resistance to PC190723 and related compounds: molecular insights from a FtsZ mutational analysis.

Kaul M, Zhang Y, Parhi AK, Lavoie EJ, Tuske S, Arnold E, Kerrigan JE, Pilch DS.

Biochimie. 2013 Oct;95(10):1880-7. doi: 10.1016/j.biochi.2013.06.010. Epub 2013 Jun 25.

19.

Macrocyclic biphenyl tetraoxazoles: synthesis, evaluation as G-quadruplex stabilizers and cytotoxic activity.

Blankson GA, Pilch DS, Liu AA, Liu LF, Rice JE, LaVoie EJ.

Bioorg Med Chem. 2013 Aug 1;21(15):4511-20. doi: 10.1016/j.bmc.2013.05.033. Epub 2013 May 30.

20.

Substituted 1,6-diphenylnaphthalenes as FtsZ-targeting antibacterial agents.

Zhang Y, Giurleo D, Parhi A, Kaul M, Pilch DS, LaVoie EJ.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2001-6. doi: 10.1016/j.bmcl.2013.02.016. Epub 2013 Feb 13.

21.

Antimicrobial activity of various 4- and 5-substituted 1-phenylnaphthalenes.

Kelley C, Lu S, Parhi A, Kaul M, Pilch DS, Lavoie EJ.

Eur J Med Chem. 2013 Feb;60:395-409. doi: 10.1016/j.ejmech.2012.12.027. Epub 2012 Dec 20.

22.

3-Phenyl substituted 6,7-dimethoxyisoquinoline derivatives as FtsZ-targeting antibacterial agents.

Kelley C, Zhang Y, Parhi A, Kaul M, Pilch DS, LaVoie EJ.

Bioorg Med Chem. 2012 Dec 15;20(24):7012-29. doi: 10.1016/j.bmc.2012.10.009. Epub 2012 Oct 17.

23.

Antibacterial activity of substituted 5-methylbenzo[c]phenanthridinium derivatives.

Parhi A, Kelley C, Kaul M, Pilch DS, LaVoie EJ.

Bioorg Med Chem Lett. 2012 Dec 1;22(23):7080-3. doi: 10.1016/j.bmcl.2012.09.097. Epub 2012 Oct 2.

24.

Antibacterial activity of substituted dibenzo[a,g]quinolizin-7-ium derivatives.

Parhi A, Lu S, Kelley C, Kaul M, Pilch DS, LaVoie EJ.

Bioorg Med Chem Lett. 2012 Nov 15;22(22):6962-6. doi: 10.1016/j.bmcl.2012.08.123. Epub 2012 Sep 20.

25.

A bactericidal guanidinomethyl biaryl that alters the dynamics of bacterial FtsZ polymerization.

Kaul M, Parhi AK, Zhang Y, LaVoie EJ, Tuske S, Arnold E, Kerrigan JE, Pilch DS.

J Med Chem. 2012 Nov 26;55(22):10160-76. doi: 10.1021/jm3012728. Epub 2012 Oct 26.

26.

Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment.

Kurtzberg LS, Roth S, Krumbholz R, Crawford J, Bormann C, Dunham S, Yao M, Rouleau C, Bagley RG, Yu XJ, Wang F, Schmid SM, Lavoie EJ, Teicher BA.

Clin Cancer Res. 2011 May 1;17(9):2777-87. doi: 10.1158/1078-0432.CCR-10-0542. Epub 2011 Mar 17.

27.

Macrocyclic hexaoxazoles: Influence of aminoalkyl substituents on RNA and DNA G-quadruplex stabilization and cytotoxicity.

Satyanarayana M, Kim YA, Rzuczek SG, Pilch DS, Liu AA, Liu LF, Rice JE, LaVoie EJ.

Bioorg Med Chem Lett. 2010 May 15;20(10):3150-4. doi: 10.1016/j.bmcl.2010.03.086. Epub 2010 Mar 30.

PMID:
20409709
28.

Macrocyclic pyridyl polyoxazoles: selective RNA and DNA G-quadruplex ligands as antitumor agents.

Rzuczek SG, Pilch DS, Liu A, Liu L, LaVoie EJ, Rice JE.

J Med Chem. 2010 May 13;53(9):3632-44. doi: 10.1021/jm1000612.

29.

A G-quadruplex stabilizer induces M-phase cell cycle arrest.

Tsai YC, Qi H, Lin CP, Lin RK, Kerrigan JE, Rzuczek SG, LaVoie EJ, Rice JE, Pilch DS, Lyu YL, Liu LF.

J Biol Chem. 2009 Aug 21;284(34):22535-43. doi: 10.1074/jbc.M109.020230. Epub 2009 Jun 16.

30.

12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents.

Feng W, Satyanarayana M, Tsai YC, Liu AA, Liu LF, LaVoie EJ.

Bioorg Med Chem. 2009 Apr 1;17(7):2877-85. doi: 10.1016/j.bmc.2009.02.023. Epub 2009 Feb 20.

31.
32.

Cytotoxicity and TOP1-targeting activity of 8- and 9-amino derivatives of 5-butyl- and 5-(2-N,N-dimethylamino)ethyl-5H-dibenzo[c,h][1,6]naphthyridin-6-ones.

Sharma L, Tsai YC, Liu AA, Liu LF, LaVoie EJ.

Eur J Med Chem. 2009 Apr;44(4):1471-6. doi: 10.1016/j.ejmech.2008.09.048. Epub 2008 Oct 11.

PMID:
19012996
33.

Bone marrow and tumor cell colony-forming units and human tumor xenograft efficacy of noncamptothecin and camptothecin topoisomerase I inhibitors.

Kurtzberg LS, Battle T, Rouleau C, Bagley RG, Agata N, Yao M, Schmid S, Roth S, Crawford J, Krumbholz R, Ewesuedo R, Yu XJ, Wang F, Lavoie EJ, Teicher BA.

Mol Cancer Ther. 2008 Oct;7(10):3212-22. doi: 10.1158/1535-7163.MCT-08-0568.

34.

Synthesis of N-substituted 5-[2-(N-alkylamino)ethyl]dibenzo[c,h][1,6]naphthyridines as novel topoisomerase I-targeting antitumor agents.

Feng W, Satyanarayana M, Cheng L, Liu A, Tsai YC, Liu LF, LaVoie EJ.

Bioorg Med Chem. 2008 Oct 15;16(20):9295-301. doi: 10.1016/j.bmc.2008.09.002. Epub 2008 Sep 5.

35.

11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents.

Feng W, Satyanarayana M, Tsai YC, Liu AA, Liu LF, LaVoie EJ.

Bioorg Med Chem. 2008 Sep 15;16(18):8598-606. doi: 10.1016/j.bmc.2008.08.018. Epub 2008 Aug 7.

36.

Syntheses and biological evaluation of topoisomerase I-targeting agents related to 11-[2-(N,N-dimethylamino)ethyl]-2,3-dimethoxy-8,9-methylenedioxy-11H-isoquino[4,3-c]cinnolin-12-one (ARC-31).

Satyanarayana M, Feng W, Cheng L, Liu AA, Tsai YC, Liu LF, LaVoie EJ.

Bioorg Med Chem. 2008 Aug 15;16(16):7824-31. doi: 10.1016/j.bmc.2008.06.046. Epub 2008 Jun 26.

PMID:
18676151
37.

Ring-closing metathesis for the synthesis of a highly G-quadruplex selective macrocyclic hexaoxazole having enhanced cytotoxic potency.

Satyanarayana M, Rzuczek SG, Lavoie EJ, Pilch DS, Liu A, Liu LF, Rice JE.

Bioorg Med Chem Lett. 2008 Jul 1;18(13):3802-4. doi: 10.1016/j.bmcl.2008.05.032. Epub 2008 May 15.

38.

Facile formation of hydrophilic derivatives of 5H-8,9-dimethoxy-5-[2-(N,N-dimethylamino)ethyl]-2,3-methylenedioxydibenzo[c,h] [1,6]naphthyridin-6-one (ARC-111) and its 12-aza analog via quaternary ammonium intermediates.

Feng W, Satyanarayana M, Tsai YC, Liu AA, Liu LF, Lavoie EJ.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3570-2. doi: 10.1016/j.bmcl.2008.05.005. Epub 2008 May 6.

PMID:
18511275
39.

Targeting human telomeric G-quadruplex DNA with oxazole-containing macrocyclic compounds.

Pilch DS, Barbieri CM, Rzuczek SG, Lavoie EJ, Rice JE.

Biochimie. 2008 Aug;90(8):1233-49. doi: 10.1016/j.biochi.2008.03.011. Epub 2008 Apr 4.

40.

Lysinyl macrocyclic hexaoxazoles: synthesis and selective G-quadruplex stabilizing properties.

Rzuczek SG, Pilch DS, LaVoie EJ, Rice JE.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):913-7. doi: 10.1016/j.bmcl.2007.12.048. Epub 2008 Jan 14.

41.

Defining the mode, energetics and specificity with which a macrocyclic hexaoxazole binds to human telomeric G-quadruplex DNA.

Barbieri CM, Srinivasan AR, Rzuczek SG, Rice JE, LaVoie EJ, Pilch DS.

Nucleic Acids Res. 2007;35(10):3272-86. Epub 2007 Apr 22.

42.

Drug self-association modulates the cellular bioavailability of DNA minor groove-directed terbenzimidazoles.

Khan QA, Barbieri CM, Srinivasan AR, Wang YH, LaVoie EJ, Pilch DS.

J Med Chem. 2006 Aug 24;49(17):5245-51.

PMID:
16913713
43.

Synthesis and G-quadruplex stabilizing properties of a series of oxazole-containing macrocycles.

Minhas GS, Pilch DS, Kerrigan JE, LaVoie EJ, Rice JE.

Bioorg Med Chem Lett. 2006 Aug 1;16(15):3891-5. Epub 2006 Jun 2.

PMID:
16735121
44.

Determination of the predominant catechins in Acacia catechu by liquid chromatography/electrospray ionization-mass spectrometry.

Shen D, Wu Q, Wang M, Yang Y, Lavoie EJ, Simon JE.

J Agric Food Chem. 2006 May 3;54(9):3219-24.

PMID:
16637676
45.

6-Substituted 6H-dibenzo[c,h][2,6]naphthyridin-5-ones: reversed lactam analogues of ARC-111 with potent topoisomerase I-targeting activity and cytotoxicity.

Zhu S, Ruchelman AL, Zhou N, Liu A, Liu LF, LaVoie EJ.

Bioorg Med Chem. 2006 May 1;14(9):3131-43. Epub 2006 Jan 18.

PMID:
16412652
46.

Esters and amides of 2,3-dimethoxy-8,9-methylenedioxy-benzo[i]phenanthridine-12-carboxylic acid: potent cytotoxic and topoisomerase I-targeting agents.

Zhu S, Ruchelman AL, Zhou N, Liu AA, Liu LF, LaVoie EJ.

Bioorg Med Chem. 2005 Dec 15;13(24):6782-94. Epub 2005 Sep 8.

PMID:
16153852
47.
48.
49.
50.

11H-Isoquino[4,3-c]cinnolin-12-ones; novel anticancer agents with potent topoisomerase I-targeting activity and cytotoxicity.

Ruchelman AL, Singh SK, Ray A, Wu X, Yang JM, Zhou N, Liu A, Liu LF, LaVoie EJ.

Bioorg Med Chem. 2004 Feb 15;12(4):795-806.

PMID:
14759740

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