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Items: 1 to 50 of 340

1.

5-Hydroxypyrido[2,3-b]pyrazin-6(5H)-one derivatives as novel dual inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H and integrase.

Sun L, Gao P, Dong G, Zhang X, Cheng X, Ding X, Wang X, Daelemans D, De Clercq E, Pannecouque C, Menéndez-Arias L, Zhan P, Liu X.

Eur J Med Chem. 2018 Jun 18;155:714-724. doi: 10.1016/j.ejmech.2018.06.036. [Epub ahead of print]

PMID:
29940462
2.

Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.

Kang D, Wang Z, Zhang H, Wu G, Zhao T, Zhou Z, Huo Z, Huang B, Feng D, Ding X, Zhang J, Zuo X, Jing L, Luo W, Guma S, Daelemans D, Clercq E, Pannecouque C, Zhan P, Liu X.

ACS Med Chem Lett. 2018 Mar 1;9(4):370-375. doi: 10.1021/acsmedchemlett.8b00054. eCollection 2018 Apr 12.

PMID:
29670703
3.

Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.

Huo Z, Zhang H, Kang D, Zhou Z, Wu G, Desta S, Zuo X, Wang Z, Jing L, Ding X, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.

ACS Med Chem Lett. 2018 Feb 27;9(4):334-338. doi: 10.1021/acsmedchemlett.7b00524. eCollection 2018 Apr 12.

PMID:
29670696
4.

Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.

Tian Y, Liu Z, Liu J, Huang B, Kang D, Zhang H, De Clercq E, Daelemans D, Pannecouque C, Lee KH, Chen CH, Zhan P, Liu X.

Eur J Med Chem. 2018 May 10;151:339-350. doi: 10.1016/j.ejmech.2018.03.059. Epub 2018 Mar 23.

PMID:
29635166
5.

The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.

Lu X, Yang J, Kang D, Gao P, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.

Bioorg Med Chem. 2018 May 1;26(8):2051-2060. doi: 10.1016/j.bmc.2018.03.003. Epub 2018 Mar 3.

PMID:
29559197
6.

Anti-HIV activity of new higher order G-quadruplex aptamers obtained from tetra-end-linked oligonucleotides.

Nici F, Oliviero G, Falanga AP, D'Errico S, Marzano M, Musumeci D, Montesarchio D, Noppen S, Pannecouque C, Piccialli G, Borbone N.

Org Biomol Chem. 2018 Mar 28;16(13):2349-2355. doi: 10.1039/C7OB02346D.

PMID:
29543291
7.

First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.

Huang B, Liu X, Tian Y, Kang D, Zhou Z, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.

Bioorg Med Chem Lett. 2018 May 1;28(8):1348-1351. doi: 10.1016/j.bmcl.2018.03.012. Epub 2018 Mar 5.

PMID:
29534929
8.

Silibinin phosphodiester glyco-conjugates: Synthesis, redox behaviour and biological investigations.

Romanucci V, Agarwal C, Agarwal R, Pannecouque C, Iuliano M, De Tommaso G, Caruso T, Di Fabio G, Zarrelli A.

Bioorg Chem. 2018 Apr;77:349-359. doi: 10.1016/j.bioorg.2018.01.026. Epub 2018 Jan 31.

PMID:
29421711
9.

Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.

Jin K, Yin H, De Clercq E, Pannecouque C, Meng G, Chen F.

Eur J Med Chem. 2018 Feb 10;145:726-734. doi: 10.1016/j.ejmech.2018.01.016. Epub 2018 Jan 8.

PMID:
29353724
10.

Discovery of novel diarylpyrimidines as potent HIV-1 NNRTIs by investigating the chemical space of a less explored "hydrophobic channel".

Zhou Z, Liu T, Kang D, Huo Z, Wu G, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.

Org Biomol Chem. 2018 Feb 7;16(6):1014-1028. doi: 10.1039/c7ob02828h.

PMID:
29349445
11.

New findings on the d(TGGGAG) sequence: Surprising anti-HIV-1 activity.

Romanucci V, Zarrelli A, Liekens S, Noppen S, Pannecouque C, Di Fabio G.

Eur J Med Chem. 2018 Feb 10;145:425-430. doi: 10.1016/j.ejmech.2018.01.005. Epub 2018 Jan 5.

PMID:
29335208
12.

Structural optimization of N1-aryl-benzimidazoles for the discovery of new non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.

Monforte AM, De Luca L, Buemi MR, Agharbaoui FE, Pannecouque C, Ferro S.

Bioorg Med Chem. 2018 Feb 1;26(3):661-674. doi: 10.1016/j.bmc.2017.12.033. Epub 2017 Dec 24.

PMID:
29291935
13.

Discovery of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the Tolerant Region I of NNIBP.

Kang D, Ding X, Wu G, Huo Z, Zhou Z, Zhao T, Feng D, Wang Z, Tian Y, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.

ACS Med Chem Lett. 2017 Oct 19;8(11):1188-1193. doi: 10.1021/acsmedchemlett.7b00361. eCollection 2017 Nov 9.

PMID:
29152052
14.

Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.

Liu Z, Tian Y, Liu J, Huang B, Kang D, De Clercq E, Daelemans D, Pannecouque C, Zhan P, Liu X.

Eur J Med Chem. 2017 Nov 10;140:383-391. doi: 10.1016/j.ejmech.2017.07.012. Epub 2017 Jul 18.

PMID:
28987601
15.

1-Hydroxypyrido[2,3-d]pyrimidin-2(1H)-ones as novel selective HIV integrase inhibitors obtained via privileged substructure-based compound libraries.

Gao P, Zhang L, Sun L, Huang T, Tan J, Zhang J, Zhou Z, Zhao T, Menéndez-Arias L, Pannecouque C, Clercq E, Zhan P, Liu X.

Bioorg Med Chem. 2017 Oct 15;25(20):5779-5789. doi: 10.1016/j.bmc.2017.09.006. Epub 2017 Sep 8.

PMID:
28951095
16.

Bioactive Natural Products Prioritization Using Massive Multi-informational Molecular Networks.

Olivon F, Allard PM, Koval A, Righi D, Genta-Jouve G, Neyts J, Apel C, Pannecouque C, Nothias LF, Cachet X, Marcourt L, Roussi F, Katanaev VL, Touboul D, Wolfender JL, Litaudon M.

ACS Chem Biol. 2017 Oct 20;12(10):2644-2651. doi: 10.1021/acschembio.7b00413. Epub 2017 Sep 15.

PMID:
28829118
17.

Discovery of novel DAPY-IAS hybrid derivatives as potential HIV-1 inhibitors using molecular hybridization based on crystallographic overlays.

Huang B, Wang X, Liu X, Chen Z, Li W, Sun S, Liu H, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.

Bioorg Med Chem. 2017 Aug 15;25(16):4397-4406. doi: 10.1016/j.bmc.2017.06.022. Epub 2017 Jun 15.

PMID:
28659246
18.

Synthesis and antiviral evaluation of base-modified deoxythreosyl nucleoside phosphonates.

Liu C, Dumbre SG, Pannecouque C, Korba B, De Jonghe S, Herdewijn P.

Org Biomol Chem. 2017 Jul 5;15(26):5513-5528. doi: 10.1039/c7ob01265a.

PMID:
28628181
19.

Searching for novel N1-substituted benzimidazol-2-ones as non-nucleoside HIV-1 RT inhibitors.

Ferro S, Buemi MR, De Luca L, Agharbaoui FE, Pannecouque C, Monforte AM.

Bioorg Med Chem. 2017 Jul 15;25(14):3861-3870. doi: 10.1016/j.bmc.2017.05.040. Epub 2017 May 19.

PMID:
28559060
20.

Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.

Kang D, Fang Z, Huang B, Lu X, Zhang H, Xu H, Huo Z, Zhou Z, Yu Z, Meng Q, Wu G, Ding X, Tian Y, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.

J Med Chem. 2017 May 25;60(10):4424-4443. doi: 10.1021/acs.jmedchem.7b00332. Epub 2017 May 15.

PMID:
28481112
21.

Chelation Motifs Affecting Metal-dependent Viral Enzymes: N'-acylhydrazone Ligands as Dual Target Inhibitors of HIV-1 Integrase and Reverse Transcriptase Ribonuclease H Domain.

Carcelli M, Rogolino D, Gatti A, Pala N, Corona A, Caredda A, Tramontano E, Pannecouque C, Naesens L, Esposito F.

Front Microbiol. 2017 Mar 20;8:440. doi: 10.3389/fmicb.2017.00440. eCollection 2017.

22.

Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.

Xue P, Lu HH, Zhu YY, Ju XL, Pannecouque C, Zheng XJ, Liu GY, Zhang XL, Gu SX.

Bioorg Med Chem Lett. 2017 Apr 15;27(8):1640-1643. doi: 10.1016/j.bmcl.2017.03.009. Epub 2017 Mar 7.

PMID:
28314598
23.

Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.

Lu HH, Xue P, Zhu YY, Ju XL, Zheng XJ, Zhang X, Xiao T, Pannecouque C, Li TT, Gu SX.

Bioorg Med Chem. 2017 Apr 15;25(8):2491-2497. doi: 10.1016/j.bmc.2017.03.009. Epub 2017 Mar 6.

PMID:
28314514
24.

Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.

Zhang H, Tian Y, Kang D, Huo Z, Zhou Z, Liu H, De Clercq E, Pannecouque C, Zhan P, Liu X.

Eur J Med Chem. 2017 Apr 21;130:209-222. doi: 10.1016/j.ejmech.2017.02.047. Epub 2017 Feb 21.

PMID:
28254696
25.

Application of the Triazolization Reaction to Afford Dihydroartemisinin Derivatives with Anti-HIV Activity.

Jana S, Iram S, Thomas J, Hayat MQ, Pannecouque C, Dehaen W.

Molecules. 2017 Feb 17;22(2). pii: E303. doi: 10.3390/molecules22020303.

26.

Structural Modifications of Diarylpyrimidine-quinolone Hybrids as Potent HIV-1 NNRTIs with an Improved Drug Resistance Profile.

Mao TQ, He QQ, Chen WX, Tang GF, Chen FE, De Clercq E, Daelemans D, Pannecouque C.

Curr Pharm Des. 2016;22(46):6982-6987. doi: 10.2174/1381612823666161122125657.

PMID:
27875973
27.

Discovery of novel piperidine-substituted indolylarylsulfones as potent HIV NNRTIs via structure-guided scaffold morphing and fragment rearrangement.

Li X, Gao P, Huang B, Zhou Z, Yu Z, Yuan Z, Liu H, Pannecouque C, Daelemans D, De Clercq E, Zhan P, Liu X.

Eur J Med Chem. 2017 Jan 27;126:190-201. doi: 10.1016/j.ejmech.2016.10.009. Epub 2016 Oct 5.

PMID:
27750153
28.

Amidate Prodrugs of Deoxythreosyl Nucleoside Phosphonates as Dual Inhibitors of HIV and HBV Replication.

Liu C, Dumbre SG, Pannecouque C, Huang C, Ptak RG, Murray MG, De Jonghe S, Herdewijn P.

J Med Chem. 2016 Oct 27;59(20):9513-9531. Epub 2016 Oct 17.

PMID:
27748590
29.

Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.

Kang D, Fang Z, Li Z, Huang B, Zhang H, Lu X, Xu H, Zhou Z, Ding X, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.

J Med Chem. 2016 Sep 8;59(17):7991-8007. doi: 10.1021/acs.jmedchem.6b00738. Epub 2016 Aug 26.

PMID:
27541578
30.

Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.

Lu X, Li X, Yang J, Huang B, Kang D, Zhao F, Zhou Z, De Clercq E, Daelemans D, Pannecouque C, Zhan P, Liu X.

Bioorg Med Chem. 2016 Sep 15;24(18):4424-4433. doi: 10.1016/j.bmc.2016.07.041. Epub 2016 Jul 21.

PMID:
27501911
31.

Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.

Chen W, Zhan P, Daelemans D, Yang J, Huang B, De Clercq E, Pannecouque C, Liu X.

Eur J Med Chem. 2016 Oct 4;121:352-363. doi: 10.1016/j.ejmech.2016.05.054. Epub 2016 May 25.

PMID:
27267005
32.

Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.

Hoshi A, Sakamoto T, Takayama J, Xuan M, Okazaki M, Hartman TL, Buckheit RW Jr, Pannecouque C, Cushman M.

Bioorg Med Chem. 2016 Jul 1;24(13):3006-3022. doi: 10.1016/j.bmc.2016.05.010. Epub 2016 May 24.

PMID:
27234889
33.

Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells.

Kulabaş N, Tatar E, Bingöl Özakpınar Ö, Özsavcı D, Pannecouque C, De Clercq E, Küçükgüzel İ.

Eur J Med Chem. 2016 Oct 4;121:58-70. doi: 10.1016/j.ejmech.2016.05.017. Epub 2016 May 7.

PMID:
27214512
34.

1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.

Geisman AN, Valuev-Elliston VT, Ozerov AA, Khandazhinskaya AL, Chizhov AO, Kochetkov SN, Pannecouque C, Naesens L, Seley-Radtke KL, Novikov MS.

Bioorg Med Chem. 2016 Jun 1;24(11):2476-85. doi: 10.1016/j.bmc.2016.04.010. Epub 2016 Apr 5.

PMID:
27112451
35.

Design, synthesis and anti-HIV activity of novel quinoxaline derivatives.

Patel SB, Patel BD, Pannecouque C, Bhatt HG.

Eur J Med Chem. 2016 Jul 19;117:230-40. doi: 10.1016/j.ejmech.2016.04.019. Epub 2016 Apr 11.

PMID:
27105027
36.

Design, synthesis, and biological evaluation of novel 5-Alkyl-6-Adamantylmethylpyrimidin-4(3H)-ones as HIV-1 non-nucleoside reverse-transcriptase inhibitors.

Li W, Huang B, Kang D, De Clercq E, Daelemans D, Pannecouque C, Zhan P, Liu X.

Chem Biol Drug Des. 2016 Sep;88(3):380-5. doi: 10.1111/cbdd.12765. Epub 2016 Jun 21.

PMID:
27062197
37.

Design, Synthesis, and Molecular Docking Studies of a Conjugated Thiadiazole-Thiourea Scaffold as Antituberculosis Agents.

Tatar E, Karakuş S, Küçükgüzel ŞG, Öktem Okullu S, Ünübol N, Kocagöz T, De Clercq E, Andrei G, Snoeck R, Pannecouque C, Kalaycı S, Şahin F, Sriram D, Yogeeswari P, Küçükgüzel İ.

Biol Pharm Bull. 2016;39(4):502-15. doi: 10.1248/bpb.b15-00698.

38.

The G-quadruplex-forming aptamer AS1411 potently inhibits HIV-1 attachment to the host cell.

Perrone R, Butovskaya E, Lago S, Garzino-Demo A, Pannecouque C, Palù G, Richter SN.

Int J Antimicrob Agents. 2016 Apr;47(4):311-6. doi: 10.1016/j.ijantimicag.2016.01.016. Epub 2016 Mar 11.

39.

Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.

Meng Q, Chen X, Kang D, Huang B, Li W, Zhan P, Daelemans D, De Clercq E, Pannecouque C, Liu X.

Eur J Med Chem. 2016 Jun 10;115:53-62. doi: 10.1016/j.ejmech.2016.02.068. Epub 2016 Mar 3.

PMID:
26994843
40.

Studies on Cycloheptathiophene-3-carboxamide Derivatives as Allosteric HIV-1 Ribonuclease H Inhibitors.

Corona A, Desantis J, Massari S, Distinto S, Masaoka T, Sabatini S, Esposito F, Manfroni G, Maccioni E, Cecchetti V, Pannecouque C, Le Grice SF, Tramontano E, Tabarrini O.

ChemMedChem. 2016 Aug 19;11(16):1709-20. doi: 10.1002/cmdc.201600015. Epub 2016 Mar 16.

PMID:
26990134
41.

Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5-b]pyridin-2-ylthioacetanilides as Potent HIV NNRTIs Via a Structure-based Bioisosterism Approach.

Li X, Huang B, Zhou Z, Gao P, Pannecouque C, Daelemans D, De Clercq E, Zhan P, Liu X.

Chem Biol Drug Des. 2016 Aug;88(2):241-53. doi: 10.1111/cbdd.12751. Epub 2016 Mar 24.

PMID:
26914186
42.

Modification of the length and structure of the linker of N(6)-benzyladenosine modulates its selective antiviral activity against enterovirus 71.

Drenichev MS, Oslovsky VE, Sun L, Tijsma A, Kurochkin NN, Tararov VI, Chizhov AO, Neyts J, Pannecouque C, Leyssen P, Mikhailov SN.

Eur J Med Chem. 2016 Mar 23;111:84-94. doi: 10.1016/j.ejmech.2016.01.036. Epub 2016 Jan 26.

PMID:
26854380
43.

The Cellular Thioredoxin-1/Thioredoxin Reductase-1 Driven Oxidoreduction Represents a Chemotherapeutic Target for HIV-1 Entry Inhibition.

Reiser K, Mathys L, Curbo S, Pannecouque C, Noppen S, Liekens S, Engman L, Lundberg M, Balzarini J, Karlsson A.

PLoS One. 2016 Jan 27;11(1):e0147773. doi: 10.1371/journal.pone.0147773. eCollection 2016.

44.

Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.

Yang J, Chen W, Kang D, Lu X, Li X, Liu Z, Huang B, Daelemans D, Pannecouque C, De Clercq E, Zhan P, Liu X.

Eur J Med Chem. 2016 Feb 15;109:294-304. doi: 10.1016/j.ejmech.2015.11.039. Epub 2015 Dec 22.

PMID:
26802545
45.

A new vinyl selenone-based domino approach to spirocyclopropyl oxindoles endowed with anti-HIV RT activity.

Palomba M, Rossi L, Sancineto L, Tramontano E, Corona A, Bagnoli L, Santi C, Pannecouque C, Tabarrini O, Marini F.

Org Biomol Chem. 2016 Feb 14;14(6):2015-24. doi: 10.1039/c5ob02451j.

PMID:
26754878
46.

Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity.

Sancineto L, Mariotti A, Bagnoli L, Marini F, Desantis J, Iraci N, Santi C, Pannecouque C, Tabarrini O.

J Med Chem. 2015 Dec 24;58(24):9601-14. doi: 10.1021/acs.jmedchem.5b01183. Epub 2015 Dec 10.

PMID:
26613134
47.

Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends.

Zhan P, Pannecouque C, De Clercq E, Liu X.

J Med Chem. 2016 Apr 14;59(7):2849-78. doi: 10.1021/acs.jmedchem.5b00497. Epub 2015 Nov 5. Review.

PMID:
26509831
48.

Human Exportin-1 is a Target for Combined Therapy of HIV and AIDS Related Lymphoma.

Boons E, Vanstreels E, Jacquemyn M, Nogueira TC, Neggers JE, Vercruysse T, van den Oord J, Tamir S, Shacham S, Landesman Y, Snoeck R, Pannecouque C, Andrei G, Daelemans D.

EBioMedicine. 2015 Aug 1;2(9):1102-13. doi: 10.1016/j.ebiom.2015.07.041. eCollection 2015 Sep.

49.

A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.

Gu SX, Qiao H, Zhu YY, Shu QC, Liu H, Ju XL, De Clercq E, Balzarini J, Pannecouque C.

Bioorg Med Chem. 2015 Oct 15;23(20):6587-93. doi: 10.1016/j.bmc.2015.09.020. Epub 2015 Sep 11.

PMID:
26385446
50.

Design, Synthesis, and Biological Evaluation of Novel 2-(Pyridin-3-yloxy)acetamide Derivatives as Potential Anti-HIV-1 Agents.

Huang B, Li X, Zhan P, De Clercq E, Daelemans D, Pannecouque C, Liu X.

Chem Biol Drug Des. 2016 Feb;87(2):283-9. doi: 10.1111/cbdd.12657. Epub 2015 Sep 29.

PMID:
26347922

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