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Items: 1 to 50 of 243

1.

Biosensor-surface plasmon resonance: A strategy to help establish a new generation RNA-specific small molecules.

Vo T, Paul A, Kumar A, Boykin DW, Wilson WD.

Methods. 2019 May 9. pii: S1046-2023(19)30049-0. doi: 10.1016/j.ymeth.2019.05.005. [Epub ahead of print]

PMID:
31077819
2.

A New Generation of Minor-Groove-Binding-Heterocyclic Diamidines That Recognize G·C Base Pairs in an AT Sequence Context.

Paul A, Guo P, Boykin DW, Wilson WD.

Molecules. 2019 Mar 7;24(5). pii: E946. doi: 10.3390/molecules24050946. Review.

3.

PU.1 controls fibroblast polarization and tissue fibrosis.

Wohlfahrt T, Rauber S, Uebe S, Luber M, Soare A, Ekici A, Weber S, Matei AE, Chen CW, Maier C, Karouzakis E, Kiener HP, Pachera E, Dees C, Beyer C, Daniel C, Gelse K, Kremer AE, Naschberger E, Stürzl M, Butter F, Sticherling M, Finotto S, Kreuter A, Kaplan MH, Jüngel A, Gay S, Nutt SL, Boykin DW, Poon GMK, Distler O, Schett G, Distler JHW, Ramming A.

Nature. 2019 Feb;566(7744):344-349. doi: 10.1038/s41586-019-0896-x. Epub 2019 Jan 30.

PMID:
30700907
4.

Heterocyclic Diamidine DNA Ligands as HOXA9 Transcription Factor Inhibitors: Design, Molecular Evaluation, and Cellular Consequences in a HOXA9-Dependant Leukemia Cell Model.

Depauw S, Lambert M, Jambon S, Paul A, Peixoto P, Nhili R, Marongiu L, Figeac M, Dassi C, Paul-Constant C, Billoré B, Kumar A, Farahat AA, Ismail MA, Mineva E, Sweat DP, Stephens CE, Boykin DW, Wilson WD, David-Cordonnier MH.

J Med Chem. 2019 Feb 14;62(3):1306-1329. doi: 10.1021/acs.jmedchem.8b01448. Epub 2019 Feb 1.

PMID:
30645099
5.

DNA recognition by linear indole-biphenyl DNA minor groove ligands.

Erlitzki N, Farahat AA, Kumar A, Boykin DW, Poon GMK.

Biophys Chem. 2019 Feb;245:6-16. doi: 10.1016/j.bpc.2018.11.004. Epub 2018 Nov 26.

PMID:
30513446
6.

Compound Shape Effects in Minor Groove Binding Affinity and Specificity for Mixed Sequence DNA.

Guo P, Farahat AA, Paul A, Harika NK, Boykin DW, Wilson WD.

J Am Chem Soc. 2018 Nov 7;140(44):14761-14769. doi: 10.1021/jacs.8b08152. Epub 2018 Oct 24.

PMID:
30353731
7.

Dynamic self-assembly of DNA minor groove-binding ligand DB921 into nanotubes triggered by an alkali halide.

Mizuta R, Devos JM, Webster J, Ling WL, Narayanan T, Round A, Munnur D, Mossou E, Farahat AA, Boykin DW, Wilson WD, Neidle S, Schweins R, Rannou P, Haertlein M, Forsyth VT, Mitchell EP.

Nanoscale. 2018 Mar 28;10(12):5550-5558. doi: 10.1039/c7nr03875e. Epub 2018 Mar 8.

8.

In Vitro and In Vivo Studies of the Trypanocidal Effect of Novel Quinolines.

Nefertiti ASG, Batista MM, Da Silva PB, Batista DGJ, Da Silva CF, Peres RB, Torres-Santos EC, Cunha-Junior EF, Holt E, Boykin DW, Brun R, Wenzler T, Soeiro MNC.

Antimicrob Agents Chemother. 2018 Jan 25;62(2). pii: e01936-17. doi: 10.1128/AAC.01936-17. Print 2018 Feb.

9.

Indole and Benzimidazole Bichalcophenes: Synthesis, DNA Binding and Antiparasitic Activity.

Farahat AA, Ismail MA, Kumar A, Wenzler T, Brun R, Paul A, Wilson WD, Boykin DW.

Eur J Med Chem. 2018 Jan 1;143:1590-1596. doi: 10.1016/j.ejmech.2017.10.056. Epub 2017 Oct 22.

10.

G-quadruplex-binding small molecules ameliorate C9orf72 FTD/ALS pathology in vitro and in vivo.

Simone R, Balendra R, Moens TG, Preza E, Wilson KM, Heslegrave A, Woodling NS, Niccoli T, Gilbert-Jaramillo J, Abdelkarim S, Clayton EL, Clarke M, Konrad MT, Nicoll AJ, Mitchell JS, Calvo A, Chio A, Houlden H, Polke JM, Ismail MA, Stephens CE, Vo T, Farahat AA, Wilson WD, Boykin DW, Zetterberg H, Partridge L, Wray S, Parkinson G, Neidle S, Patani R, Fratta P, Isaacs AM.

EMBO Mol Med. 2018 Jan;10(1):22-31. doi: 10.15252/emmm.201707850.

11.

Pharmacological inhibition of the transcription factor PU.1 in leukemia.

Antony-Debré I, Paul A, Leite J, Mitchell K, Kim HM, Carvajal LA, Todorova TI, Huang K, Kumar A, Farahat AA, Bartholdy B, Narayanagari SR, Chen J, Ambesi-Impiombato A, Ferrando AA, Mantzaris I, Gavathiotis E, Verma A, Will B, Boykin DW, Wilson WD, Poon GM, Steidl U.

J Clin Invest. 2017 Dec 1;127(12):4297-4313. doi: 10.1172/JCI92504. Epub 2017 Oct 30.

12.

Antileishmanial Efficacy and Pharmacokinetics of DB766-Azole Combinations.

Joice AC, Yang S, Farahat AA, Meeds H, Feng M, Li J, Boykin DW, Wang MZ, Werbovetz KA.

Antimicrob Agents Chemother. 2017 Dec 21;62(1). pii: e01129-17. doi: 10.1128/AAC.01129-17. Print 2018 Jan.

13.

A modular design for minor groove binding and recognition of mixed base pair sequences of DNA.

Guo P, Paul A, Kumar A, Harika NK, Wang S, Farahat AA, Boykin DW, Wilson WD.

Chem Commun (Camb). 2017 Sep 25;53(75):10406-10409. doi: 10.1039/c7cc06246j. Epub 2017 Sep 7.

14.

Phenotypic evaluation and in silico ADMET properties of novel arylimidamides in acute mouse models of Trypanosoma cruzi infection.

da Silva CF, Batista DDGJ, de Araújo JS, Cunha-Junior EF, Stephens CE, Banerjee M, Farahat AA, Akay S, Fisher MK, Boykin DW, Soeiro MNC.

Drug Des Devel Ther. 2017 Apr 3;11:1095-1105. doi: 10.2147/DDDT.S120618. eCollection 2017.

15.

Investigation of the electrostatic and hydration properties of DNA minor groove-binding by a heterocyclic diamidine by osmotic pressure.

Erlitzki N, Huang K, Xhani S, Farahat AA, Kumar A, Boykin DW, Poon GMK.

Biophys Chem. 2017 Dec;231:95-104. doi: 10.1016/j.bpc.2017.02.008. Epub 2017 Mar 20.

16.

In Vitro, Ex Vivo, and In Vivo Activities of Diamidines against Trypanosoma congolense and Trypanosoma vivax.

Gillingwater K, Kunz C, Braghiroli C, Boykin DW, Tidwell RR, Brun R.

Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02356-16. doi: 10.1128/AAC.02356-16. Print 2017 May.

17.

Exploration of DAPI analogues: Synthesis, antitrypanosomal activity, DNA binding and fluorescence properties.

Farahat AA, Kumar A, Say M, Wenzler T, Brun R, Paul A, Wilson WD, Boykin DW.

Eur J Med Chem. 2017 Mar 10;128:70-78. doi: 10.1016/j.ejmech.2017.01.037. Epub 2017 Jan 24.

18.

Systematic synthetic and biophysical development of mixed sequence DNA binding agents.

Paul A, Kumar A, Nanjunda R, Farahat AA, Boykin DW, Wilson WD.

Org Biomol Chem. 2017 Jan 25;15(4):827-835. doi: 10.1039/c6ob02390h.

19.

Synthesis, DNA binding and antitrypanosomal activity of benzimidazole analogues of DAPI.

Farahat AA, Bennett-Vaughn C, Mineva EM, Kumar A, Wenzler T, Brun R, Liu Y, Wilson WD, Boykin DW.

Bioorg Med Chem Lett. 2016 Dec 15;26(24):5907-5910. doi: 10.1016/j.bmcl.2016.11.006. Epub 2016 Nov 3.

PMID:
27843114
20.

The Thiophene "Sigma-Hole" as a Concept for Preorganized, Specific Recognition of G⋅C Base Pairs in the DNA Minor Groove.

Guo P, Paul A, Kumar A, Farahat AA, Kumar D, Wang S, Boykin DW, Wilson WD.

Chemistry. 2016 Oct 17;22(43):15404-15412. doi: 10.1002/chem.201603422. Epub 2016 Sep 14.

21.

Lithium Hexamethyldisilazane Transformation of Transiently Protected 4-Aza/Benzimidazole Nitriles to Amidines and their Dimethyl Sulfoxide Mediated Imidazole Ring Formation.

Abou-Elkhair RA, Hassan AE, Boykin DW, Wilson WD.

Org Lett. 2016 Sep 16;18(18):4714-7. doi: 10.1021/acs.orglett.6b02359. Epub 2016 Sep 8.

22.

Antiprion Activity of DB772 and Related Monothiophene- and Furan-Based Analogs in a Persistently Infected Ovine Microglia Culture System.

Dinkel KD, Stanton JB, Boykin DW, Stephens CE, Madsen-Bouterse SA, Schneider DA.

Antimicrob Agents Chemother. 2016 Aug 22;60(9):5467-82. doi: 10.1128/AAC.00811-16. Print 2016 Sep.

23.

Phenotypic Screening In Vitro of Novel Aromatic Amidines against Trypanosoma cruzi.

Simões-Silva MR, Nefertiti AS, De Araújo JS, Batista MM, Da Silva PB, Bahia MT, Menna-Barreto RS, Pavão BP, Green J, Farahat AA, Kumar A, Boykin DW, Soeiro MN.

Antimicrob Agents Chemother. 2016 Jul 22;60(8):4701-7. doi: 10.1128/AAC.01788-15. Print 2016 Aug.

24.

Imino proton NMR guides the reprogramming of A•T specific minor groove binders for mixed base pair recognition.

Harika NK, Paul A, Stroeva E, Chai Y, Boykin DW, Germann MW, Wilson WD.

Nucleic Acids Res. 2016 Jun 2;44(10):4519-27. doi: 10.1093/nar/gkw353. Epub 2016 Apr 29.

25.

Pharmacologic efficacy of PU.1 inhibition by heterocyclic dications: a mechanistic analysis.

Stephens DC, Kim HM, Kumar A, Farahat AA, Boykin DW, Poon GM.

Nucleic Acids Res. 2016 May 19;44(9):4005-13. doi: 10.1093/nar/gkw229. Epub 2016 Apr 13.

26.

Synthesis and pharmacological evaluation of mono-arylimidamides as antileishmanial agents.

Zhu X, Farahat AA, Mattamana M, Joice A, Pandharkar T, Holt E, Banerjee M, Gragg JL, Hu L, Kumar A, Yang S, Wang MZ, Boykin DW, Werbovetz KA.

Bioorg Med Chem Lett. 2016 May 15;26(10):2551-2556. doi: 10.1016/j.bmcl.2016.03.082. Epub 2016 Mar 25.

27.

Pentamidine analogs as inhibitors of [(3)H]MK-801 and [(3)H]ifenprodil binding to rat brain NMDA receptors.

Berger ML, Maciejewska D, Vanden Eynde JJ, Mottamal M, Żabiński J, Kaźmierczak P, Rezler M, Jarak I, Piantanida I, Karminski-Zamola G, Mayence A, Rebernik P, Kumar A, Ismail MA, Boykin DW, Huang TL.

Bioorg Med Chem. 2015 Aug 1;23(15):4489-500. doi: 10.1016/j.bmc.2015.06.012. Epub 2015 Jun 14.

28.

Mixed up minor groove binders: Convincing A·T specific compounds to recognize a G·C base pair.

Paul A, Nanjunda R, Kumar A, Laughlin S, Nhili R, Depauw S, Deuser SS, Chai Y, Chaudhary AS, David-Cordonnier MH, Boykin DW, Wilson WD.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4927-4932. doi: 10.1016/j.bmcl.2015.05.005. Epub 2015 May 19.

29.

Resolution of mixed site DNA complexes with dimer-forming minor-groove binders by using electrospray ionization mass spectrometry: compound structure and DNA sequence effects.

Laughlin S, Wang S, Kumar A, Farahat AA, Boykin DW, Wilson WD.

Chemistry. 2015 Mar 27;21(14):5528-39. doi: 10.1002/chem.201406322. Epub 2015 Feb 20.

30.

Chemotherapy of second stage human African trypanosomiasis: comparison between the parenteral diamidine DB829 and its oral prodrug DB868 in vervet monkeys.

Thuita JK, Wolf KK, Murilla GA, Bridges AS, Boykin DW, Mutuku JN, Liu Q, Jones SK, Gem CO, Ching S, Tidwell RR, Wang MZ, Paine MF, Brun R.

PLoS Negl Trop Dis. 2015 Feb 5;9(2):e0003409. doi: 10.1371/journal.pntd.0003409. eCollection 2015 Feb.

31.

Bis-benzimidazole hits against Naegleria fowleri discovered with new high-throughput screens.

Rice CA, Colon BL, Alp M, Göker H, Boykin DW, Kyle DE.

Antimicrob Agents Chemother. 2015 Apr;59(4):2037-44. doi: 10.1128/AAC.05122-14. Epub 2015 Jan 20.

32.

Understanding mixed sequence DNA recognition by novel designed compounds: the kinetic and thermodynamic behavior of azabenzimidazole diamidines.

Paul A, Chai Y, Boykin DW, Wilson WD.

Biochemistry. 2015 Jan 20;54(2):577-87. doi: 10.1021/bi500989r. Epub 2014 Dec 24.

33.

A novel approach using electrospray ionization mass spectrometry to study competitive binding of small molecules with mixed DNA sequences.

Laughlin S, Wang S, Kumar A, Boykin DW, Wilson WD.

Anal Bioanal Chem. 2014 Oct;406(25):6441-5. doi: 10.1007/s00216-014-8044-9. Epub 2014 Jul 30.

34.

Synthesis and antiparasitic activity of new bis-arylimidamides: DB766 analogs modified in the terminal groups.

Liu ZY, Wenzler T, Brun R, Zhu X, Boykin DW.

Eur J Med Chem. 2014 Aug 18;83:167-73. doi: 10.1016/j.ejmech.2014.06.022. Epub 2014 Jun 12.

PMID:
24956553
35.

In vitro and in vivo evaluation of 28DAP010, a novel diamidine for treatment of second-stage African sleeping sickness.

Wenzler T, Yang S, Patrick DA, Braissant O, Ismail MA, Tidwell RR, Boykin DW, Wang MZ, Brun R.

Antimicrob Agents Chemother. 2014 Aug;58(8):4452-63. doi: 10.1128/AAC.02309-13. Epub 2014 May 27.

36.

Pharmacokinetic comparison to determine the mechanisms underlying the differential efficacies of cationic diamidines against first- and second-stage human African trypanosomiasis.

Yang S, Wenzler T, Miller PN, Wu H, Boykin DW, Brun R, Wang MZ.

Antimicrob Agents Chemother. 2014 Jul;58(7):4064-74. doi: 10.1128/AAC.02605-14. Epub 2014 May 5.

37.

In vitro investigation of the efficacy of novel diamidines against Trypanosoma cruzi.

Timm BL, Da Silva PB, Batista MM, Farahat AA, Kumar A, Boykin DW, Soeiro MN.

Parasitology. 2014 Sep;141(10):1272-6. doi: 10.1017/S0031182014000407. Epub 2014 Apr 15.

PMID:
24735493
38.

In vitro and in vivo studies of the biological activity of novel arylimidamides against Trypanosoma cruzi.

De Araújo JS, Da Silva CF, Batista DG, Da Silva PB, Meuser MB, Aiub CA, da Silva MF, Araújo-Lima CF, Banerjee M, Farahat AA, Stephens CE, Kumar A, Boykin DW, Soeiro MN.

Antimicrob Agents Chemother. 2014 Jul;58(7):4191-5. doi: 10.1128/AAC.01403-13. Epub 2014 Mar 3.

39.

The unusual monomer recognition of guanine-containing mixed sequence DNA by a dithiophene heterocyclic diamidine.

Munde M, Kumar A, Peixoto P, Depauw S, Ismail MA, Farahat AA, Paul A, Say MV, David-Cordonnier MH, Boykin DW, Wilson WD.

Biochemistry. 2014 Feb 25;53(7):1218-27. doi: 10.1021/bi401582t. Epub 2014 Feb 13.

40.

Design and synthesis of heterocyclic cations for specific DNA recognition: from AT-rich to mixed-base-pair DNA sequences.

Chai Y, Paul A, Rettig M, Wilson WD, Boykin DW.

J Org Chem. 2014 Feb 7;79(3):852-66. doi: 10.1021/jo402599s. Epub 2014 Jan 21.

41.

Green fluorescent diamidines as diagnostic probes for trypanosomes.

Giordani F, Munde M, Wilson WD, Ismail MA, Kumar A, Boykin DW, Barrett MP.

Antimicrob Agents Chemother. 2014;58(3):1793-6. doi: 10.1128/AAC.02024-13. Epub 2013 Dec 23.

42.

Structure-dependent binding of arylimidamides to the DNA minor groove.

Chai Y, Munde M, Kumar A, Mickelson L, Lin S, Campbell NH, Banerjee M, Akay S, Liu Z, Farahat AA, Nhili R, Depauw S, David-Cordonnier MH, Neidle S, Wilson WD, Boykin DW.

Chembiochem. 2014 Jan 3;15(1):68-79. doi: 10.1002/cbic.201300622. Epub 2013 Dec 9.

43.

Discovery of new G-quadruplex binding chemotypes.

Ohnmacht SA, Varavipour E, Nanjunda R, Pazitna I, Di Vita G, Gunaratnam M, Kumar A, Ismail MA, Boykin DW, Wilson WD, Neidle S.

Chem Commun (Camb). 2014 Jan 28;50(8):960-3. doi: 10.1039/c3cc48616h.

44.

CYP1A1 and CYP1B1-mediated biotransformation of the antitrypanosomal methamidoxime prodrug DB844 forms novel metabolites through intramolecular rearrangement.

Ju W, Yang S, Ansede JH, Stephens CE, Bridges AS, Voyksner RD, Ismail MA, Boykin DW, Tidwell RR, Hall JE, Wang MZ.

J Pharm Sci. 2014 Jan;103(1):337-49. doi: 10.1002/jps.23765. Epub 2013 Nov 1.

45.

Structure-dependent inhibition of the ETS-family transcription factor PU.1 by novel heterocyclic diamidines.

Munde M, Wang S, Kumar A, Stephens CE, Farahat AA, Boykin DW, Wilson WD, Poon GM.

Nucleic Acids Res. 2014 Jan;42(2):1379-90. doi: 10.1093/nar/gkt955. Epub 2013 Oct 23.

46.

Effect of treatment with a cationic antiviral compound on acute infection with bovine viral diarrhea virus.

Newcomer BW, Marley MS, Galik PK, Zhang Y, Riddell KP, Boykin DW, Kumar A, Kuhnt LA, Gard JA, Givens MD.

Can J Vet Res. 2013 Jul;77(3):170-6.

47.

Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.

Hu L, Patel A, Bondada L, Yang S, Wang MZ, Munde M, Wilson WD, Wenzler T, Brun R, Boykin DW.

Bioorg Med Chem. 2013 Nov 1;21(21):6732-41. doi: 10.1016/j.bmc.2013.08.006. Epub 2013 Aug 13.

48.

Pharmacokinetics, Trypanosoma brucei gambiense efficacy, and time of drug action of DB829, a preclinical candidate for treatment of second-stage human African trypanosomiasis.

Wenzler T, Yang S, Braissant O, Boykin DW, Brun R, Wang MZ.

Antimicrob Agents Chemother. 2013 Nov;57(11):5330-43. doi: 10.1128/AAC.00398-13. Epub 2013 Aug 19.

49.

Different thermodynamic signatures for DNA minor groove binding with changes in salt concentration and temperature.

Wang S, Kumar A, Aston K, Nguyen B, Bashkin JK, Boykin DW, Wilson WD.

Chem Commun (Camb). 2013 Oct 4;49(76):8543-5. doi: 10.1039/c3cc44569k.

50.

Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.

Patrick DA, Bakunov SA, Bakunova SM, Jones SK, Wenzler T, Barszcz T, Kumar A, Boykin DW, Werbovetz KA, Brun R, Tidwell RR.

Eur J Med Chem. 2013 Sep;67:310-24. doi: 10.1016/j.ejmech.2013.06.033. Epub 2013 Jun 25.

PMID:
23871911

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