M Witvrouw

Summary

Affiliation: Katholieke Universiteit Leuven
Country: Belgium

Publications

  1. pmc 1,1,3-Trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine (TTD) derivatives: a new class of nonnucleoside human immunodeficiency virus type 1 (HIV-1) reverse transcriptase inhibitors with anti-HIV-1 activity
    M Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 42:618-23. 1998
  2. ncbi request reprint Potent and selective inhibition of HIV and SIV by prostratin interacting with viral entry
    Myriam Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Antivir Chem Chemother 14:321-8. 2003
  3. ncbi request reprint Susceptibility of HIV-2, SIV and SHIV to various anti-HIV-1 compounds: implications for treatment and postexposure prophylaxis
    Myriam Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Antivir Ther 9:57-65. 2004
  4. ncbi request reprint Polyanionic (i.e., polysulfonate) dendrimers can inhibit the replication of human immunodeficiency virus by interfering with both virus adsorption and later steps (reverse transcriptase/integrase) in the virus replicative cycle
    M Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 58:1100-8. 2000
  5. pmc SRR-SB3, a disulfide-containing macrolide that inhibits a late stage of the replicative cycle of human immunodeficiency virus
    M Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 41:262-8. 1997
  6. ncbi request reprint Conversion of 2',3'-dideoxyadenosine (ddA) and 2',3'-didehydro-2',3'-dideoxyadenosine (d4A) to their corresponding aryloxyphosphoramidate derivatives markedly potentiates their activity against human immunodeficiency virus and hepatitis B virus
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    FEBS Lett 410:324-8. 1997
  7. ncbi request reprint Mutations in the non-nucleoside binding-pocket interfere with the multi-nucleoside resistance phenotype
    K Van Laethem
    Rega Institute for Medical Research and University Hospitals, Katholieke Universiteit Leuven, Belgium
    AIDS 15:553-61. 2001
  8. ncbi request reprint A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 57:116-24. 2000
  9. ncbi request reprint Viral entry as the primary target for the anti-HIV activity of chicoric acid and its tetra-acetyl esters
    W Pluymers
    Rega Institute for Medical Research, K U Leuven, Leuven, Belgium
    Mol Pharmacol 58:641-8. 2000
  10. pmc Prevalence and characteristics of multinucleoside-resistant human immunodeficiency virus type 1 among European patients receiving combinations of nucleoside analogues
    K Van Vaerenbergh
    Rega Institute for Medical Research and University Hospitals, Leuven, Belgium
    Antimicrob Agents Chemother 44:2109-17. 2000

Collaborators

Detail Information

Publications61

  1. pmc 1,1,3-Trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine (TTD) derivatives: a new class of nonnucleoside human immunodeficiency virus type 1 (HIV-1) reverse transcriptase inhibitors with anti-HIV-1 activity
    M Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 42:618-23. 1998
    ..Modelling studies suggest that in contrast to most other NNRTIs, but akin to nevirapine, QM96521 does not act as a hydrogen bond donor in the RT-drug complex...
  2. ncbi request reprint Potent and selective inhibition of HIV and SIV by prostratin interacting with viral entry
    Myriam Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Antivir Chem Chemother 14:321-8. 2003
    ..We concluded that prostratin inhibits the entry step of the replication cycle of HIV by interacting with a cellular target necessary for viral entry...
  3. ncbi request reprint Susceptibility of HIV-2, SIV and SHIV to various anti-HIV-1 compounds: implications for treatment and postexposure prophylaxis
    Myriam Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Antivir Ther 9:57-65. 2004
    ..Co-receptor antagonists such as AMD3100 show promising anti-HIV-2 therapeutic modalities. Both AMD3100 and enfuvirtide could be used for prophylaxis against SHIV89.6...
  4. ncbi request reprint Polyanionic (i.e., polysulfonate) dendrimers can inhibit the replication of human immunodeficiency virus by interfering with both virus adsorption and later steps (reverse transcriptase/integrase) in the virus replicative cycle
    M Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 58:1100-8. 2000
    ..e., V2, V3, and C3, V4, and C4 regions) of the BRI2923-resistant NL4.3 strains that were not present in the wild-type NL4.3 strain, whereas no mutations were found in the reverse transcriptase or integrase genes...
  5. pmc SRR-SB3, a disulfide-containing macrolide that inhibits a late stage of the replicative cycle of human immunodeficiency virus
    M Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 41:262-8. 1997
    ..Time-of-addition experiments indicated that SRR-SB3 acts at a late stage of the HIV-1 replicative cycle...
  6. ncbi request reprint Conversion of 2',3'-dideoxyadenosine (ddA) and 2',3'-didehydro-2',3'-dideoxyadenosine (d4A) to their corresponding aryloxyphosphoramidate derivatives markedly potentiates their activity against human immunodeficiency virus and hepatitis B virus
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    FEBS Lett 410:324-8. 1997
    ..Both Cf 1001 and Cf 1093 were equally efficient as 3TC (lamivudine) in inhibiting HBV replication in hepatocytes, and rank among the most potent HIV and HBV inhibitors reported so far in cell culture...
  7. ncbi request reprint Mutations in the non-nucleoside binding-pocket interfere with the multi-nucleoside resistance phenotype
    K Van Laethem
    Rega Institute for Medical Research and University Hospitals, Katholieke Universiteit Leuven, Belgium
    AIDS 15:553-61. 2001
    ..CONCLUSION: Changes in the non-nucleoside binding pocket must affect the conformation of residues at the dNTP binding site, and can result in a partial phenotypic reversal of the multi-nucleoside resistance phenotype...
  8. ncbi request reprint A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 57:116-24. 2000
    ..Mechanism of action studies revealed that CGP64222 can inhibit the HIV replicative cycle, also through a selective interaction with the CXC-chemokine receptor 4 coreceptor...
  9. ncbi request reprint Viral entry as the primary target for the anti-HIV activity of chicoric acid and its tetra-acetyl esters
    W Pluymers
    Rega Institute for Medical Research, K U Leuven, Leuven, Belgium
    Mol Pharmacol 58:641-8. 2000
    ..Although inhibition of HIV integrase activity by L-CA and its derivatives was confirmed in an oligonucleotide-driven assay, integrase carrying the G140S mutation was inhibited to the same extent as the wild-type integrase...
  10. pmc Prevalence and characteristics of multinucleoside-resistant human immunodeficiency virus type 1 among European patients receiving combinations of nucleoside analogues
    K Van Vaerenbergh
    Rega Institute for Medical Research and University Hospitals, Leuven, Belgium
    Antimicrob Agents Chemother 44:2109-17. 2000
    ..MNR HIV-1 is found only among multinucleoside-experienced patients. Its prevalence is low in Europe, but it should be closely monitored since it seriously limits treatment options...
  11. ncbi request reprint S-adenosylhomocysteine hydrolase inhibitors interfere with the replication of human immunodeficiency virus type 1 through inhibition of the LTR transactivation
    D Daelemans
    Rega Institute for Medical Research, Katholieke Universtiteit Leuven, Belgium
    Mol Pharmacol 52:1157-63. 1997
    ..Our results suggest that AdoHcy hydrolase and the associated S-adenosylmethionine-dependent methylation mechanism play a role in the process of long terminal repeat transactivation and, hence, HIV replication...
  12. ncbi request reprint Potent anti-HIV (type 1 and type 2) activity of polyoxometalates: structure-activity relationship and mechanism of action
    M Witvrouw
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium, USA
    J Med Chem 43:778-83. 2000
    ....
  13. ncbi request reprint Highly favorable antiviral activity and resistance profile of the novel thiocarboxanilide pentenyloxy ether derivatives UC-781 and UC-82 as inhibitors of human immunodeficiency virus type 1 replication
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Mol Pharmacol 50:394-401. 1996
    ....
  14. ncbi request reprint Selection of human immunodeficiency virus type 1 resistance against the pyranodipyrimidine V-165 points to a multimodal mechanism of action
    A Hombrouck
    Laboratory for Molecular Virology and Drug Discovery, Katholieke Universiteit Leuven, Leuven, Flanders, Belgium
    J Antimicrob Chemother 59:1084-95. 2007
    ..As part of pre-clinical studies with PDP, we wanted to investigate HIV resistance development against V-165 and to further characterize the physicochemical properties of the compound...
  15. ncbi request reprint In vitro evaluation of the effect of temporary removal of HIV drug pressure
    M Witvrouw
    Rega Institute for Medical Research, K U Leuven, Belgium
    Antiviral Res 46:215-21. 2000
    ..Consequently, virus rebounded when drug therapy stopped. In conclusion, our findings suggest that drug holidays would result in viral breakthrough, even after virus replication has been previously suppressed by adequate drug levels...
  16. ncbi request reprint Long-term stability of human immunodeficiency virus viral load and infectivity in whole blood
    A M Vandamme
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Eur J Clin Invest 29:445-52. 1999
    ..We intended to evaluate the stability of human immunodeficiency virus (HIV) type 1 virions in whole blood and in culture medium...
  17. pmc Inhibition of human immunodeficiency virus type 1 integration by diketo derivatives
    Wim Pluymers
    Rega Institute for Medical Research, K U Leuven, Minderbroedersstraat 10, Belgium
    Antimicrob Agents Chemother 46:3292-7. 2002
    ..In cell culture, addition of L-708,906 could be postponed for 7 h after infection, a moment coinciding with HIV integration. Inhibition of integration in cell culture was confirmed by quantitative Alu-PCR...
  18. pmc Development of resistance against diketo derivatives of human immunodeficiency virus type 1 by progressive accumulation of integrase mutations
    Valery Fikkert
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    J Virol 77:11459-70. 2003
    ..As to the replication kinetics of the selected strains, the replication fitness for all strains was lower than that of the wild-type HIV-1 strain...
  19. ncbi request reprint Novel inhibitors of HIV-1 integration
    M Witvrouw
    Rega Institute for Medical Research, Minderbroedersstraat 10, B 3000 Leuven, Flanders, Belgium
    Curr Drug Metab 5:291-304. 2004
    ..Furthermore, we will describe the two classes of integrase inhibitors and discuss their antiviral activity, molecular mechanism of anti-HIV action and the selection of HIV resistance against these drugs...
  20. pmc Antiretroviral activities of acyclic nucleoside phosphonates [9-(2-phosphonylmethoxyethyl)adenine, 9-(2-phosphonylmethoxyethyl)guanine, (R)-9-(2-phosphonylmethoxypropyl)adenine, and MDL 74,968] in cell cultures and murine sarcoma virus-infected newborn NM
    J Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 41:611-6. 1997
    ..Treatment of the NMRI mice with PMEA, (R)-PMPA, and MDL 74,968 at 25 or 50 mg/kg resulted in a high percentage of long-term survivors...
  21. ncbi request reprint In search of authentic inhibitors of HIV-1 integration
    Zeger Debyser
    Rega Institute for Medical Research, KU Leuven, Flanders, Belgium
    Antivir Chem Chemother 13:1-15. 2002
    ..We point to potential pitfalls in defining an inhibitor as an authentic integrase inhibitor, and propose new strategies and technologies for the discovery of authentic HIV integration inhibitors...
  22. pmc Virus evolution reveals an exclusive role for LEDGF/p75 in chromosomal tethering of HIV
    Anneleen Hombrouck
    The Laboratory for Molecular Virology and Gene Therapy, KULeuven and IRC KULAK, Leuven, Flanders, Belgium
    PLoS Pathog 3:e47. 2007
    ..Moreover, the role of LEDGF/p75 in targeting integration will stimulate research on strategies to direct gene therapy vectors into safe landing sites...
  23. ncbi request reprint New class of HIV integrase inhibitors that block viral replication in cell culture
    Christophe Pannecouque
    Rega Institute for Medical Research, KULeuven, Minderbroedersstraat 10, Belgium
    Curr Biol 12:1169-77. 2002
    ....
  24. ncbi request reprint N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action
    Irene M Lagoja
    Laboratory of Medicinal Chemistry, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, Belgium
    J Med Chem 46:1546-53. 2003
    ....
  25. ncbi request reprint Multiple mutations in human immunodeficiency virus-1 integrase confer resistance to the clinical trial drug S-1360
    Valery Fikkert
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    AIDS 18:2019-28. 2004
    ..Study of HIV-1 resistance development to the diketo analogue S-1360, the first HIV-1 integrase strand transfer inhibitor that has entered clinical development...
  26. ncbi request reprint Mutations in both env and gag genes are required for HIV-1 resistance to the polysulfonic dendrimer SPL2923, as corroborated by chimeric virus technology
    Anke Hantson
    Laboratory for Molecular Virology, Molecular Medicine, Katholieke Universiteit Leuven, Flanders, Belgium
    Antivir Chem Chemother 16:253-66. 2005
    ..Phenotypic analysis of the NL4.3/SPL2923 p17- and p17/gp160-recombined strains indicated that the mutations in both env and gag have to be present to fully reproduce the resistance of NL4.3/SPL2923 towards SPL2923...
  27. pmc Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors
    Anneleen Hombrouck
    Division of Molecular Medicine, Katholieke Universiteit Leuven, Flanders, Belgium
    Antimicrob Agents Chemother 52:2861-9. 2008
    ..Transport studies with Caco cells suggest a low oral bioavailability...
  28. pmc env chimeric virus technology for evaluating human immunodeficiency virus susceptibility to entry inhibitors
    Valery Fikkert
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium
    Antimicrob Agents Chemother 46:3954-62. 2002
    ..In addition, we obtained a proof of principle that env CVT can become a helpful diagnostic tool in assessments of the phenotypic resistance of clinical HIV isolates to HIV entry inhibitors...
  29. ncbi request reprint Synthesis and anti-HIV evaluation of the novel 2-(m-chlorobenzyl)-4-substituted-7-methyl-1, 1, 3-trioxo-pyrazolo[4, 5-e] [1, 2, 4]thiadiazines
    Ren zhang Yan
    Institute of Medicinal Chemistry, School of Pharmacy, Shandong University, 250012 Jinan, China
    Arch Pharm Res 29:957-62. 2006
    ..Compound (7a) showed activity against HIV-1-induced cytopathicity, with an EC50 value of 45.6 microM, but none of the compounds exhibited inhibitory activity against HIV-2...
  30. pmc Discovery of a small-molecule HIV-1 integrase inhibitor-binding site
    Laith Q Al-Mawsawi
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90089, USA
    Proc Natl Acad Sci U S A 103:10080-5. 2006
    ..This type of structural information can help illuminate processes of inhibitor resistance and thereby facilitate the design of more potent second-generation inhibitors...
  31. ncbi request reprint Synthesis and anti-HIV-1 and anti-HCMV activity of 1-substituted 3-(3,5-dimethylbenzyl)uracil derivatives
    Tokumi Maruyama
    Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokushima Bunri University, Shido, Samuki, Japan
    Chem Pharm Bull (Tokyo) 54:325-33. 2006
    ..These results were confirmed by Docking Studies using the program, Glide ligand docking jobs, which suggests hydrogen bonding between amide N-H of Lys 101 and nitrogen of the cyanomethyl and picolyl group...
  32. doi request reprint A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series
    Laura De Luca
    Dipartimento Farmaco Chimico, Universita di Messina, Viale Annunziata, 98168 Messina, Italy
    Bioorg Med Chem Lett 18:2891-5. 2008
    ..The synthesis of the new designed molecules is also described...
  33. pmc Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137
    Anneleen Hombrouck
    Division of Molecular Medicine, Katholieke Universiteit Leuven, B 3000 Leuven
    Antimicrob Agents Chemother 52:2069-78. 2008
    ..These data may have implications for cross-resistance of different integrase inhibitors in the clinic...
  34. doi request reprint Synthesis and anti-HIV activity evaluation of novel 2,4-disubstituted 7-methyl-1,1,3-trioxo-2,4-dihydro-pyrazolo-[4,5-e][1,2]thiadiazines
    Xin Yong Liu
    Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan, PR China
    Arch Pharm (Weinheim) 341:216-22. 2008
    ..The most active HIV-2 inhibitor was compound 7i (R1 = benzyl, R2 = 4-t-butyl-benzyl) with an EC50 value of 18.7 microM and SI=15, which may provide a useful lead for further molecular optimization...
  35. doi request reprint Reaction of rosmarinic acid with nitrite ions in acidic conditions: discovery of nitro- and dinitrorosmarinic acids as new anti-HIV-1 agents
    Melanie Dubois
    Laboratoire de Chimie Organique et Macromoléculaire, UMR CNRS 8009, Universite de Lille 1, 59655 Villeneuve d Ascq, France
    J Med Chem 51:2575-9. 2008
    ..The nitration of rosmarinic acid strongly improves the anti-integrase inhibition and the antiviral activity without increasing the cellular toxicity...
  36. ncbi request reprint New 4-[(1-benzyl-1H-indol-3-yl)carbonyl]-3-hydroxyfuran-2(5H)-ones, beta-diketo acid analogs as HIV-1 integrase inhibitors
    Stefania Ferro
    Dipartimento Farmaco Chimico, Universita di Messina, Messina, Italy
    Arch Pharm (Weinheim) 340:292-8. 2007
    ..The microwave-assisted synthesis was employed in some steps of the chemical procedures...
  37. doi request reprint Quinolone 3-carboxylic acid pharmacophore: design of second generation HIV-1 integrase inhibitors
    Raveendra Dayam
    Department of Pharmacology and Pharmaceutical Sciences, University of Southern California, Los Angeles, California 90089, USA
    J Med Chem 51:1136-44. 2008
    ....
  38. ncbi request reprint Novel virtual screening protocol based on the combined use of molecular modeling and electron-ion interaction potential techniques to design HIV-1 integrase inhibitors
    Cristina Tintori
    Dipartimento Farmaco Chimico Tecnologico, Universita degli Studi di Siena, Via Alcide de Gasperi 2, I 53100 Siena, Italy
    J Chem Inf Model 47:1536-44. 2007
    ..Biological investigations also showed, in agreement with modeling studies, that these compounds prevent recognition of DNA by IN in a fluorescence fluctuation assay, probably by interacting with the DNA binding domain of IN...
  39. ncbi request reprint Synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole as potential HIV-1 NNRTIs
    Jingde Wu
    Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No 44, Wenhuaxi Road, Jinan, 250012, PR China
    Molecules 12:2003-16. 2007
    ..Compound 4e was found to be the most active inhibitor against HIV-1 replication in cell culture (EC50 = 12 microM) and against HIV-1 reverse transcriptase (IC50 = 43.5 microM), which provided a good lead for further optimization...
  40. pmc Transient and stable knockdown of the integrase cofactor LEDGF/p75 reveals its role in the replication cycle of human immunodeficiency virus
    Linos Vandekerckhove
    Molecular Medicine, K U Leuven and IRC KULAK, Kapucijnenvoer 33, B 3000 Leuven, Flanders, Belgium
    J Virol 80:1886-96. 2006
    ..Altogether, our data validate LEDGF/p75 as an important cellular cofactor for HIV integration and as a potential target for antiviral drug development...
  41. ncbi request reprint Pharmacophore-based design of HIV-1 integrase strand-transfer inhibitors
    Maria Letizia Barreca
    Dipartimento Farmaco Chimico, Universita di Messina, Viale Annunziata, 98168 Messina, Italy
    J Med Chem 48:7084-8. 2005
    ..96. The resulting pharmacophore model guided the rational design of benzylindoles as new potent IN inhibitors, whose microwave-assisted synthesis and biological evaluation are reported...
  42. ncbi request reprint Evaluation of the anti-HIV activity of statins
    Gemma Moncunill
    Retrovirology Laboratory IrsiCaixa and HIV Unit, Hospital Universitari Germans Trias i Pujol, Universitat Autonoma de Barcelona, 08916 Badalona, Spain
    AIDS 19:1697-700. 2005
    ..No anti-HIV activity was detected at subtoxic concentrations and simvastatin did not induce a significant change in the mean viral load or CD4 cell count in study patients. We caution on the use of statins as antiretroviral agents...
  43. pmc Resistance of human immunodeficiency virus type 1 to the high-mannose binding agents cyanovirin N and concanavalin A
    Myriam Witvrouw
    Department of Clinical Virology, University of Goteborg, Guldhedsgatan 10B, S 413 46 Goteborg, Sweden
    J Virol 79:7777-84. 2005
    ....
  44. ncbi request reprint Integrase mutants defective for interaction with LEDGF/p75 are impaired in chromosome tethering and HIV-1 replication
    Stephane Emiliani
    Institut Cochin, U567 INSERM, UPR8104 CNRS, Université Paris VI et VII, Tour 43, 2e etage, couloir 43 44, 2 place Jussieu, F 75251 Paris Cedex 05, France
    J Biol Chem 280:25517-23. 2005
    ..Furthermore, we found that LEDGF/p75 tethers HIV-1 integrase to chromosomes and that this interaction may be important for the integration process and the replication of HIV-1...
  45. ncbi request reprint Efficient 3D database screening for novel HIV-1 IN inhibitors
    Maria Letizia Barreca
    Dipartimento Farmaco Chimico, Universita di Messina, Viale Annunziata, 98168 Messina, Italy
    J Chem Inf Comput Sci 44:1450-5. 2004
    ..Biological testing shows that our strategy was successful in searching for new structural leads as HIV-1 IN inhibitors...
  46. ncbi request reprint Synthesis and antiviral activity of 1,3-disubstituted uracils against HIV-1 and HCMV
    Tokumi Maruyama
    Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Tokushima, Japan
    Antivir Chem Chemother 14:271-9. 2003
    ..We found that 1-benzyl-3-(3,5-dimethylbenzyl)uracil and 1-cyanomethyl-3-(3,5-dimethylbenzyl)-4-thiouracil showed powerful inhibition against HCMV and HIV-1, respectively...
  47. ncbi request reprint Anti-HIV activity of thiosemicarbazone and semicarbazone derivatives of (+/-)-3-menthone
    Vibha Mishra
    Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi 221005, India
    Arch Pharm (Weinheim) 335:183-6. 2002
    ..The studies revealed that maximum protection is offered by chloro-substituted derivatives 2 and 7 against HIV-1 (III(B)) and HIV-2 (ROD)...
  48. ncbi request reprint Synthesis and antiviral activity evaluation of some new 6-substituted 3-(1-adamantyl)-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles
    Marina Kritsanida
    Department of Pharmacy, University of Athens, Greece
    Farmaco 57:253-7. 2002
    ..No antiviral effects were noted with any of the compounds at subtoxic concentrations in cell culture...
  49. ncbi request reprint Chemical studies of essential oils of Juniperus oxycedrus ssp. badia
    Sofia Salido
    Departamento de Quimica Inorganica y Organica, Facultad de Ciencias Experimentales, Universidad de Jaen, 23071 Jaen, Spain
    J Ethnopharmacol 81:129-34. 2002
    ....
  50. ncbi request reprint Synthesis and biological activity of some 4-substituted 1-[1-(2,3-dihydroxy-1-propoxy)methyl-1,2,3-triazol-(4 & 5)-ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines
    Omar Moukha-chafiq
    Laboratoire de Chimie Bio Organique, Faculte des Sciences, Agadir, Morocco
    Farmaco 57:27-32. 2002
    ..No marked activity was found...
  51. ncbi request reprint Synthesis of new covalently bound kappa-carrageenan-AZT conjugates with improved anti-HIV activities
    Patrick Vlieghe
    Laboratoire de Chimie Biomoleculaire, Faculte des Sciences de Luminy, 163 Avenue de Luminy, Case 901, 13288 Marseille Cedex 9, France
    J Med Chem 45:1275-83. 2002
    ..Moreover, kappa-carrageenan is a well-tolerated biopolymer, already used in the food industry...
  52. ncbi request reprint New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation
    Antonios Kolocouris
    School of Pharmacy, Department of Pharmaceutical Chemistry, University of Athens, Panepistimioupoli Zografou, GR 15771, Athens, Greece
    Bioorg Med Chem Lett 12:723-7. 2002
    ..Whether this difference in structure can be correlated with the biological activity will be investigated in future studies...
  53. ncbi request reprint Antiviral activity of 3-(3,5-dimethylbenzyl)uracil derivatives against HIV-1 and HCMV
    Tokumi Maruyama
    Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokushima Bunri University, Kagawa, Japan
    Nucleosides Nucleotides Nucleic Acids 26:1553-8. 2007
    ..1-Arylmethyl derivatives also exhibited good anti-HIV-1 activity; and that of the 2- and 4-picolyl derivatives was particularly excellent...
  54. ncbi request reprint Synthesis and anti-HIV evaluation of novel 1,3-disubstituted thieno[3,2-c][1,2,6]thiadiazin-4(3H)-one 2,2-dioxides(TTDDs)
    Yongqiang Lin
    Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No 44 Wenhuaxi Road, Jinan 250012, China
    Bioorg Med Chem 16:157-63. 2008
    ..0 microM and a selectivity index (SI) of >76. The structure-activity relationship (SAR) is discussed...
  55. ncbi request reprint Polysulfonates derived from metal thiolate complexes as inhibitors of HIV-1 and various other enveloped viruses in vitro
    Donald E Bergstrom
    Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Ind, USA
    Antivir Chem Chemother 13:185-95. 2002
    ..Based on these results, the platinum and palladium compounds appear to be promising candidates for further studies, that is, as vaginal microbicides in the prevention of genital HIV and/or HSV transmission...
  56. ncbi request reprint Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors
    Laith Q Al-Mawsawi
    Department of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90089, USA
    Bioorg Med Chem Lett 17:6472-5. 2007
    ..The novel hydrazides displayed low micromolar IN inhibitory activity and are several hundred-fold less cytotoxic than previously disclosed salicylhydrazide IN inhibitors...
  57. ncbi request reprint Toward novel HIV-1 integrase binding inhibitors: molecular modeling, synthesis, and biological studies
    Claudia Mugnaini
    Dipartimento Farmaco Chimico Tecnologico, Universita degli Studi di Siena, Via A De Gasperi 2, I 53100 Siena, Italy
    Bioorg Med Chem Lett 17:5370-3. 2007
    ..A small family of structurally related molecules has been synthesized and biologically evaluated with one of the compounds showing an IC(50)=12 microM...
  58. ncbi request reprint Are 5'-O-carbamate-2',3'-dideoxythiacytidine new anti-HIV and anti-HBV nucleoside drugs or prodrugs?
    Carole Anastasi
    Laboratoire de Chimie Biomoleculaire, INSERM U 382, IBDM, Universite Mediterranee, Parc Scientifique de Luminy, 163 Avenue de Luminy, Case 901, 13288 Marseille Cedex 9, France
    Bioorg Med Chem Lett 13:2459-63. 2003
    ..The antiviral properties as well as the mechanism of action of 3TC analogues have been studied and evaluated...
  59. ncbi request reprint Synthesis and antiviral activities of 3-aralkylthiomethylimidazo[1,2-b]pyridazine derivatives
    Christophe Galtier
    Laboratoire de Chimie Therapeutique, Faculte de Pharmacie, Tours, France
    Antivir Chem Chemother 14:177-82. 2003
    ..The results presented here suggest that compound 10 should be considered as a new lead in the development of antiviral agents...
  60. ncbi request reprint Heterocyclic rimantadine analogues with antiviral activity
    George Stamatiou
    Department of Pharmacy, University of Athens, Panepistimioupoli Zografou, GR 15771 Athens, Greece
    Bioorg Med Chem 11:5485-92. 2003
    ..Substitution of piperidine 10 with a dialkyaminoethyl group led to the active compounds 15a and 15b: compound 15a was active against influenza A virus whereas both 15a and 15b were active against HIV-1...
  61. doi request reprint Investigations on the 4-quinolone-3-carboxylic acid motif. 1. Synthesis and structure-activity relationship of a class of human immunodeficiency virus type 1 integrase inhibitors
    Serena Pasquini
    Dipartimento Farmaco Chimico Tecnologico, Universita degli Studi di Siena, Via A Moro, 53100 Siena, Italy
    J Med Chem 51:5125-9. 2008
    ..Some of the new compounds proved to be able to inhibit the strand transfer step of the virus integration process in the micromolar range. Docking studies and quantum mechanics calculations were used to rationalize these data...