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Items: 1 to 50 of 155

1.

Antivirals in medical biodefense.

Bugert JJ, Hucke F, Zanetta P, Bassetto M, Brancale A.

Virus Genes. 2020 Feb 19. doi: 10.1007/s11262-020-01737-5. [Epub ahead of print] Review.

PMID:
32076918
2.

A new antiviral scaffold for human norovirus identified with computer-aided approaches on the viral polymerase.

Giancotti G, Rigo I, Pasqualetto G, Young MT, Neyts J, Rocha-Pereira J, Brancale A, Ferla S, Bassetto M.

Sci Rep. 2019 Dec 5;9(1):18413. doi: 10.1038/s41598-019-54903-7.

3.

The ying and yang of idebenone: Not too little, not too much - cell death in NQO1 deficient cells and the mouse retina.

Varricchio C, Beirne K, Heard C, Newland B, Rozanowska M, Brancale A, Votruba M.

Free Radic Biol Med. 2019 Nov 24. pii: S0891-5849(19)32186-0. doi: 10.1016/j.freeradbiomed.2019.11.030. [Epub ahead of print]

PMID:
31775023
4.

The repositioning of epigenetic probes/inhibitors identifies new anti-schistosomal lead compounds and chemotherapeutic targets.

Whatley KCL, Padalino G, Whiteland H, Geyer KK, Hulme BJ, Chalmers IW, Forde-Thomas J, Ferla S, Brancale A, Hoffmann KF.

PLoS Negl Trop Dis. 2019 Nov 15;13(11):e0007693. doi: 10.1371/journal.pntd.0007693. eCollection 2019 Nov.

5.

Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.

Romagnoli R, Oliva P, Salvador MK, Camacho ME, Padroni C, Brancale A, Ferla S, Hamel E, Ronca R, Grillo E, Bortolozzi R, Rruga F, Mariotto E, Viola G.

Eur J Med Chem. 2019 Nov 1;181:111577. doi: 10.1016/j.ejmech.2019.111577. Epub 2019 Aug 1.

PMID:
31400707
6.

Fluoxetine Inhibits Enterovirus Replication by Targeting the Viral 2C Protein in a Stereospecific Manner.

Bauer L, Manganaro R, Zonsics B, Strating JRPM, El Kazzi P, Lorenzo Lopez M, Ulferts R, van Hoey C, Maté MJ, Langer T, Coutard B, Brancale A, van Kuppeveld FJM.

ACS Infect Dis. 2019 Sep 13;5(9):1609-1623. doi: 10.1021/acsinfecdis.9b00179. Epub 2019 Jul 31.

7.

Erratum to 'Combining bioinformatics, cheminformatics, functional genomics and whole organism approaches for identifying epigenetic drug targets in Schistosoma mansoni' [IJP Drugs Drug Resist. 8 (2018) 559-570].

Padalino G, Ferla S, Brancale A, Chalmers IW, Hoffmann KF.

Int J Parasitol Drugs Drug Resist. 2019 Aug;10:91. doi: 10.1016/j.ijpddr.2019.07.001. Epub 2019 Jul 2. No abstract available.

8.

A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF5) and pentafluoroethyl (C2F5) substituents: Improved antiproliferative agents against prostate cancer.

Pertusati F, Ferla S, Bassetto M, Brancale A, Khandil S, Westwell AD, McGuigan C.

Eur J Med Chem. 2019 Oct 15;180:1-14. doi: 10.1016/j.ejmech.2019.07.001. Epub 2019 Jul 3.

PMID:
31288149
9.

A novel interaction between dengue virus nonstructural protein 1 and the NS4A-2K-4B precursor is required for viral RNA replication but not for formation of the membranous replication organelle.

Płaszczyca A, Scaturro P, Neufeldt CJ, Cortese M, Cerikan B, Ferla S, Brancale A, Pichlmair A, Bartenschlager R.

PLoS Pathog. 2019 May 9;15(5):e1007736. doi: 10.1371/journal.ppat.1007736. eCollection 2019 May.

10.

Targeting the Viral Polymerase of Diarrhea-Causing Viruses as a Strategy to Develop a Single Broad-Spectrum Antiviral Therapy.

Bassetto M, Van Dycke J, Neyts J, Brancale A, Rocha-Pereira J.

Viruses. 2019 Feb 20;11(2). pii: E173. doi: 10.3390/v11020173. Review.

11.

Synthesis, in vitro and in vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents.

Morigi R, Locatelli A, Leoni A, Rambaldi M, Bortolozzi R, Mattiuzzo E, Ronca R, Maccarinelli F, Hamel E, Bai R, Brancale A, Viola G.

Eur J Med Chem. 2019 Mar 15;166:514-530. doi: 10.1016/j.ejmech.2019.01.049. Epub 2019 Jan 26.

PMID:
30784885
12.

Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.

Romagnoli R, Prencipe F, Oliva P, Baraldi S, Baraldi PG, Schiaffino Ortega S, Chayah M, Kimatrai Salvador M, Lopez-Cara LC, Brancale A, Ferla S, Hamel E, Ronca R, Bortolozzi R, Mariotto E, Mattiuzzo E, Viola G.

J Med Chem. 2019 Feb 14;62(3):1274-1290. doi: 10.1021/acs.jmedchem.8b01391. Epub 2019 Jan 18.

PMID:
30633509
13.

Combining bioinformatics, cheminformatics, functional genomics and whole organism approaches for identifying epigenetic drug targets in Schistosoma mansoni.

Padalino G, Ferla S, Brancale A, Chalmers IW, Hoffmann KF.

Int J Parasitol Drugs Drug Resist. 2018 Dec;8(3):559-570. doi: 10.1016/j.ijpddr.2018.10.005. Epub 2018 Nov 13. Erratum in: Int J Parasitol Drugs Drug Resist. 2019 Aug;10:91.

14.

3-Aryl/Heteroaryl-5-amino-1-(3',4',5'-trimethoxybenzoyl)-1,2,4-triazoles as antimicrotubule agents. Design, synthesis, antiproliferative activity and inhibition of tubulin polymerization.

Romagnoli R, Prencipe F, Oliva P, Baraldi S, Baraldi PG, Brancale A, Ferla S, Hamel E, Bortolozzi R, Viola G.

Bioorg Chem. 2018 Oct;80:361-374. doi: 10.1016/j.bioorg.2018.06.037. Epub 2018 Jun 30.

PMID:
29986184
15.

Structure-activity relationship study of itraconazole, a broad-range inhibitor of picornavirus replication that targets oxysterol-binding protein (OSBP).

Bauer L, Ferla S, Head SA, Bhat S, Pasunooti KK, Shi WQ, Albulescu L, Liu JO, Brancale A, van Kuppeveld FJM, Strating JRPM.

Antiviral Res. 2018 Aug;156:55-63. doi: 10.1016/j.antiviral.2018.05.010. Epub 2018 May 26.

16.

In silico screening for human norovirus antivirals reveals a novel non-nucleoside inhibitor of the viral polymerase.

Ferla S, Netzler NE, Ferla S, Veronese S, Tuipulotu DE, Guccione S, Brancale A, White PA, Bassetto M.

Sci Rep. 2018 Mar 7;8(1):4129. doi: 10.1038/s41598-018-22303-y.

17.

Rational modifications on a benzylidene-acrylohydrazide antiviral scaffold, synthesis and evaluation of bioactivity against Chikungunya virus.

Giancotti G, Cancellieri M, Balboni A, Giustiniano M, Novellino E, Delang L, Neyts J, Leyssen P, Brancale A, Bassetto M.

Eur J Med Chem. 2018 Apr 10;149:56-68. doi: 10.1016/j.ejmech.2018.02.054. Epub 2018 Feb 23.

PMID:
29499487
18.

The Molecular Determinants of Small-Molecule Ligand Binding at P2X Receptors.

Pasqualetto G, Brancale A, Young MT.

Front Pharmacol. 2018 Feb 2;9:58. doi: 10.3389/fphar.2018.00058. eCollection 2018.

19.

Design, synthesis and evaluation against Chikungunya virus of novel small-molecule antiviral agents.

Tardugno R, Giancotti G, De Burghgraeve T, Delang L, Neyts J, Leyssen P, Brancale A, Bassetto M.

Bioorg Med Chem. 2018 Feb 15;26(4):869-874. doi: 10.1016/j.bmc.2018.01.002. Epub 2018 Jan 6.

PMID:
29336951
20.

Synthesis and biological evaluation of 6-substituted-5-fluorouridine ProTides.

Slusarczyk M, Ferla S, Brancale A, McGuigan C.

Bioorg Med Chem. 2018 Feb 1;26(3):551-565. doi: 10.1016/j.bmc.2017.11.037. Epub 2017 Dec 2.

PMID:
29277307
21.

2-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition.

Romagnoli R, Kimatrai Salvador M, Schiaffino Ortega S, Baraldi PG, Oliva P, Baraldi S, Lopez-Cara LC, Brancale A, Ferla S, Hamel E, Balzarini J, Liekens S, Mattiuzzo E, Basso G, Viola G.

Eur J Med Chem. 2018 Jan 1;143:683-698. doi: 10.1016/j.ejmech.2017.11.096.

22.

Networks of enzymatically oxidized membrane lipids support calcium-dependent coagulation factor binding to maintain hemostasis.

Lauder SN, Allen-Redpath K, Slatter DA, Aldrovandi M, O'Connor A, Farewell D, Percy CL, Molhoek JE, Rannikko S, Tyrrell VJ, Ferla S, Milne GL, Poole AW, Thomas CP, Obaji S, Taylor PR, Jones SA, de Groot PG, Urbanus RT, Hörkkö S, Uderhardt S, Ackermann J, Vince Jenkins P, Brancale A, Krönke G, Collins PW, O'Donnell VB.

Sci Signal. 2017 Nov 28;10(507). pii: eaan2787. doi: 10.1126/scisignal.aan2787.

23.

Small molecules targeted to the microtubule-Hec1 interaction inhibit cancer cell growth through microtubule stabilization.

Ferrara M, Sessa G, Fiore M, Bernard F, Asteriti IA, Cundari E, Colotti G, Ferla S, Desideri M, Buglioni S, Trisciuoglio D, Del Bufalo D, Brancale A, Degrassi F.

Oncogene. 2018 Jan 11;37(2):231-240. doi: 10.1038/onc.2017.320. Epub 2017 Sep 18.

24.

Virtual Screening of Acyclovir Derivatives as Potential Antiviral Agents: Design, Synthesis, and Biological Evaluation of New Acyclic Nucleoside ProTides.

Derudas M, Vanpouille C, Carta D, Zicari S, Andrei G, Snoeck R, Brancale A, Margolis L, Balzarini J, McGuigan C.

J Med Chem. 2017 Sep 28;60(18):7876-7896. doi: 10.1021/acs.jmedchem.7b01009. Epub 2017 Sep 19.

25.

Editorial.

Brancale A.

Antivir Chem Chemother. 2017 Aug;25(2):19. doi: 10.1177/2040206617724304. No abstract available.

26.

Broad-spectrum non-nucleoside inhibitors for caliciviruses.

Netzler NE, Enosi Tuipulotu D, Eltahla AA, Lun JH, Ferla S, Brancale A, Urakova N, Frese M, Strive T, Mackenzie JM, White PA.

Antiviral Res. 2017 Oct;146:65-75. doi: 10.1016/j.antiviral.2017.07.014. Epub 2017 Jul 27.

PMID:
28757394
27.

Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.

Famiglini V, La Regina G, Coluccia A, Masci D, Brancale A, Badia R, Riveira-Muñoz E, Esté JA, Crespan E, Brambilla A, Maga G, Catalano M, Limatola C, Formica FR, Cirilli R, Novellino E, Silvestri R.

J Med Chem. 2017 Aug 10;60(15):6528-6547. doi: 10.1021/acs.jmedchem.6b01906. Epub 2017 Jul 5.

PMID:
28628334
28.

Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents.

Bassetto M, Ferla S, Giancotti G, Pertusati F, Westwell AD, Brancale A, McGuigan C.

Medchemcomm. 2017 May 26;8(7):1414-1420. doi: 10.1039/c7md00164a. eCollection 2017 Jul 1.

29.

3-Aroyl-1,4-diarylpyrroles Inhibit Chronic Myeloid Leukemia Cell Growth through an Interaction with Tubulin.

La Regina G, Bai R, Coluccia A, Famiglini V, Passacantilli S, Naccarato V, Ortar G, Mazzoccoli C, Ruggieri V, Agriesti F, Piccoli C, Tataranni T, Nalli M, Brancale A, Vultaggio S, Mercurio C, Varasi M, Saponaro C, Sergio S, Maffia M, Coluccia AML, Hamel E, Silvestri R.

ACS Med Chem Lett. 2017 Apr 26;8(5):521-526. doi: 10.1021/acsmedchemlett.7b00022. eCollection 2017 May 11.

30.

Editorial for AVCC relaunch issue.

Brancale A.

Antivir Chem Chemother. 2017 Apr;25(1):1. doi: 10.1177/2040206617704930. No abstract available.

31.

Synthesis and Biological Evaluation of 2-Methyl-4,5-Disubstituted Oxazoles as a Novel Class of Highly Potent Antitubulin Agents.

Romagnoli R, Baraldi PG, Prencipe F, Oliva P, Baraldi S, Salvador MK, Lopez-Cara LC, Brancale A, Ferla S, Hamel E, Ronca R, Bortolozzi R, Mariotto E, Porcù E, Basso G, Viola G.

Sci Rep. 2017 Apr 13;7:46356. doi: 10.1038/srep46356.

32.

Therapeutically targeting guanylate cyclase-C: computational modeling of plecanatide, a uroguanylin analog.

Brancale A, Shailubhai K, Ferla S, Ricci A, Bassetto M, Jacob GS.

Pharmacol Res Perspect. 2017 Mar 12;5(2):e00295. doi: 10.1002/prp2.295. eCollection 2017 Apr.

33.

Kinase-independent phosphoramidate S1P1 receptor agonist benzyl ether derivatives.

James E, Pertusati F, Brancale A, McGuigan C.

Bioorg Med Chem Lett. 2017 Mar 15;27(6):1371-1378. doi: 10.1016/j.bmcl.2017.02.011. Epub 2017 Feb 9.

PMID:
28236593
34.

Shape-based virtual screening, synthesis and evaluation of novel pyrrolone derivatives as antiviral agents against HCV.

Bassetto M, Leyssen P, Neyts J, Yerukhimovich MM, Frick DN, Brancale A.

Bioorg Med Chem Lett. 2017 Feb 15;27(4):936-940. doi: 10.1016/j.bmcl.2016.12.087. Epub 2017 Jan 3.

PMID:
28089348
35.

Synthesis and evaluation of 5-(1H-indol-3-yl)-N-aryl-1,3,4-oxadiazol-2-amines as Bcl-2 inhibitory anticancer agents.

Hamdy R, Ziedan NI, Ali S, Bordoni C, El-Sadek M, Lashin E, Brancale A, Jones AT, Westwell AD.

Bioorg Med Chem Lett. 2017 Feb 15;27(4):1037-1040. doi: 10.1016/j.bmcl.2016.12.061. Epub 2016 Dec 27.

PMID:
28087272
36.

Virtual screening, SAR, and discovery of 5-(indole-3-yl)-2-[(2-nitrophenyl)amino] [1,3,4]-oxadiazole as a novel Bcl-2 inhibitor.

Ziedan NI, Hamdy R, Cavaliere A, Kourti M, Prencipe F, Brancale A, Jones AT, Westwell AD.

Chem Biol Drug Des. 2017 Jul;90(1):147-155. doi: 10.1111/cbdd.12936. Epub 2017 Feb 24.

PMID:
28067996
37.

Discovery of novel multi-target indole-based derivatives as potent and selective inhibitors of chikungunya virus replication.

Scuotto M, Abdelnabi R, Collarile S, Schiraldi C, Delang L, Massa A, Ferla S, Brancale A, Leyssen P, Neyts J, Filosa R.

Bioorg Med Chem. 2017 Jan 1;25(1):327-337. doi: 10.1016/j.bmc.2016.10.037. Epub 2016 Oct 31.

PMID:
27856239
38.

ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites.

Kandil S, Balzarini J, Rat S, Brancale A, Westwell AD, McGuigan C.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5618-5623. doi: 10.1016/j.bmcl.2016.10.077. Epub 2016 Oct 27.

39.

Novel symmetrical phenylenediamines as potential anti-hepatitis C virus agents.

Bassetto M, Ferla S, Leyssen P, Neyts J, Yerukhimovich MM, Frick DN, O'Donnell R, Brancale A.

Antivir Chem Chemother. 2015 Dec;24(5-6):155-160. doi: 10.1177/2040206616676353. Epub 2016 Nov 4.

40.

In silico identification, design and synthesis of novel piperazine-based antiviral agents targeting the hepatitis C virus helicase.

Bassetto M, Leyssen P, Neyts J, Yerukhimovich MM, Frick DN, Courtney-Smith M, Brancale A.

Eur J Med Chem. 2017 Jan 5;125:1115-1131. doi: 10.1016/j.ejmech.2016.10.043. Epub 2016 Oct 23.

PMID:
27810598
41.

Structural biology in antiviral drug discovery.

Bassetto M, Massarotti A, Coluccia A, Brancale A.

Curr Opin Pharmacol. 2016 Oct;30:116-130. doi: 10.1016/j.coph.2016.08.014. Epub 2016 Sep 6. Review.

PMID:
27611878
42.

Discovery of novel dengue virus NS5 methyltransferase non-nucleoside inhibitors by fragment-based drug design.

Benmansour F, Trist I, Coutard B, Decroly E, Querat G, Brancale A, Barral K.

Eur J Med Chem. 2017 Jan 5;125:865-880. doi: 10.1016/j.ejmech.2016.10.007. Epub 2016 Oct 5.

PMID:
27750202
43.

Impairment of cocaine-mediated behaviours in mice by clinically relevant Ras-ERK inhibitors.

Papale A, Morella IM, Indrigo MT, Bernardi RE, Marrone L, Marchisella F, Brancale A, Spanagel R, Brambilla R, Fasano S.

Elife. 2016 Aug 24;5. pii: e17111. doi: 10.7554/eLife.17111.

44.

Computer-aided identification, synthesis and evaluation of substituted thienopyrimidines as novel inhibitors of HCV replication.

Bassetto M, Leyssen P, Neyts J, Yerukhimovich MM, Frick DN, Brancale A.

Eur J Med Chem. 2016 Nov 10;123:31-47. doi: 10.1016/j.ejmech.2016.07.035. Epub 2016 Jul 19.

PMID:
27474921
45.

Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.

Ferla S, Bassetto M, Pertusati F, Kandil S, Westwell AD, Brancale A, McGuigan C.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3636-40. doi: 10.1016/j.bmcl.2016.06.001. Epub 2016 Jun 2.

PMID:
27301368
46.

Design and Synthesis of Potent in Vitro and in Vivo Anticancer Agents Based on 1-(3',4',5'-Trimethoxyphenyl)-2-Aryl-1H-Imidazole.

Romagnoli R, Baraldi PG, Prencipe F, Oliva P, Baraldi S, Tabrizi MA, Lopez-Cara LC, Ferla S, Brancale A, Hamel E, Ronca R, Bortolozzi R, Mariotto E, Basso G, Viola G.

Sci Rep. 2016 May 24;6:26602. doi: 10.1038/srep26602.

47.

Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.

Bassetto M, Ferla S, Pertusati F, Kandil S, Westwell AD, Brancale A, McGuigan C.

Eur J Med Chem. 2016 Aug 8;118:230-43. doi: 10.1016/j.ejmech.2016.04.052. Epub 2016 Apr 22.

48.

Identification of novel 2-(1H-indol-1-yl)-benzohydrazides CXCR4 ligands impairing breast cancer growth and motility.

Grande F, Barone I, Aiello F, Brancale A, Cancellieri M, Badolato M, Chemi F, Giordano C, Vircillo V, Bonofiglio D, Garofalo A, Andò S, Catalano S.

Future Med Chem. 2016;8(2):93-106. doi: 10.4155/fmc.15.176. Epub 2016 Jan 25.

PMID:
26807787
49.

Quercetin derivatives as novel antihypertensive agents: Synthesis and physiological characterization.

Grande F, Parisi OI, Mordocco RA, Rocca C, Puoci F, Scrivano L, Quintieri AM, Cantafio P, Ferla S, Brancale A, Saturnino C, Cerra MC, Sinicropi MS, Angelone T.

Eur J Pharm Sci. 2016 Jan 20;82:161-70. doi: 10.1016/j.ejps.2015.11.021. Epub 2015 Dec 2.

PMID:
26631584
50.

Base damage, local sequence context and TP53 mutation hotspots: a molecular dynamics study of benzo[a]pyrene induced DNA distortion and mutability.

Menzies GE, Reed SH, Brancale A, Lewis PD.

Nucleic Acids Res. 2015 Oct 30;43(19):9133-46. doi: 10.1093/nar/gkv910. Epub 2015 Sep 22.

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