72 Result(s)

Article

Synthesis and anti-HIV evaluation of new 2-Thioxoimidazolidin-4-ones and their Arylidine (styryl) derivatives

1,3-Bis{(2-thiophene-2-yl)ethyl}-5-(arylidine)-2-thioxoimidazolidin-4-ones (5a – 5 m) have been synthesized by condensation of 1,3-diarylalkyl-2-thiohydantoin (4) with various aromatic aldehydes. Compound (4) was...

D. H. Mahajan, K. H. Chikhalia, C. Pannecouque… in Pharmaceutical Chemistry Journal (2012)

Chapter

Antiviral Agents Acting as DNA or RNA Chain Terminators

Nucleoside or nucleotide analogue inhibitors of viral replication almost act as chain terminators during DNA (DNA- and retroviruses) or RNA (RNA viruses) synthesis. Following intracellular phosphorylation, by ...

E. De Clercq, J. Neyts in Antiviral Strategies (2009)

Article

Ovine Skin Organotypic Cultures Applied to the Ex vivo Study of Orf Virus Infection

A. Scagliarini, F. Dal Pozzo, L. Gallina, A. Guercio… in Veterinary Research Communications (2005)

Article

9-(2-Aryloxyethyl) Derivatives of Adenine - a New Class of Non-nucleosidic Antiviral Agents

New 9-(aryloxyalkyl) derivatives of adenine have been prepared by alkylation of adenine with tosylates, bromides, and α-chloro ethers containing terminal aromatic fragments in anhydrous DMF in the presence of ...

V. I. Petrov, A. A. Ozerov, M. S. Novikov… in Chemistry of Heterocyclic Compounds (2003)

Article

Pronounced cytostatic activity and bystander effect of a novel series of fluorescent tricyclic acyclovir and ganciclovir derivatives in herpes simplex virus thymidine kinase gene-transduced tumor cell lines

A number of tricyclic acyclovir (ACV) and ganciclovir (GCV) derivatives substituted with bulky lipophilic groups have been identified as potent and highly selective cytostatic agents against herpes simplex vir...

J Balzarini, T Ostrowski, T Goslinski, E De Clercq, B Golankiewicz in Gene Therapy (2002)

Article

Selection of HSV-1 TK gene-transfected murine mammary carcinoma cells resistant to (E)-5-(2-bromovinyl)-2′-deoxyuridine (BVDU) and ganciclovir (GCV)

We evaluated the molecular mechanism of resistance in herpes simplex virus type 1 (HSV-1) thymidine kinase (TK) gene-transfected murine mammary carcinoma (FM3ATK⁻/HSV-1 TK⁺) cells, that were selected for resistan...

B Degrève, E De Clercq, J Balzarini in Gene Therapy (2000)

Article

Bystander effect of purine nucleoside analogues in HSV-1tk suicide gene therapy is superior to that of pyrimidine nucleoside analogues

Introduction of the herpes simplex virus type 1 thymidine kinase gene into tumor cells, followed by the administration of the antiherpes nucleoside analogue ganciclovir has been demonstrated to be effective in...

B Degrève, E De Clercq, J Balzarini in Gene Therapy (1999)

Article

Carrier Mechanisms Involved in the Transepithelial Transport of bis(POM)-PMEA and Its Metabolites Across Caco-2 Monolayers

Purpose. To investigate the role of carrier mechanisms in: [1] the polarized transport of the bis(pivaloyloxymethyl)- [bis(POM)-] ester prodrug of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine [PMEA] a...

P. Annaert, J. Van Gelder, L. Naesens, E. De Clercq… in Pharmaceutical Research (1998)

Article

Superior cytostatic activity of the ganciclovir elaidic acid ester due to the prolonged intracellular retention of ganciclovir anabolites in herpes simplex virus type 1 thymidine kinase gene-transfected tumor cells

Ganciclovir (GCV) and its lipophilic elaidic acid ester prodrug E-GCV were evaluated for their antiherpetic, cytostatic and metabolic properties. E-GCV proved exquisitely inhibitory to the replication of herpe...

J Balzarini, B Degrève, G Andrei, J Neyts, M Sandvold, F Myhren… in Gene Therapy (1998)

Article

Comparison of the Disposition of Ester Prodrugs of the Antiviral Agent 9-(2-phosphonylmethoxyethyl)adenine [PMEA] in Caco-2 Monolayers

Purpose. To evaluate the potential of several bis-ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA, adefovir) to enhance the oral absorption of PMEA.

P. Annaert, G. Gosselin, A. Pompon, S. Benzaria, G. Valette… in Pharmaceutical Research (1998)

Chapter

Metabolism of Eicar (5-Ethynyl-1-β-D- Ribofuranosylimidazole-4-Carboxamide),A Potent Inhibitor of Inosinate Dehydrogenase

The cytostatic agent 5-ethynyl-l-β-D-ribofuranosylimidazole-4-carboxamide (EICAR) causes a rapid and marked inhibition of inosinate (IMP) dehydrogenase activity in intact tumor cells. [³H]EICAR is metabolised in ...

J. Balzarini, L. Stet, A. Matsuda, L. Wiebe… in Purine and Pyrimidine Metabolism in Man IX (1998)

Chapter

Metabolism and Anti-HIV Activity of Phosphoramidate Derivatives of D4T-MP with Variations in the Amino Acid Moiety

The metabolism of different phosphoramidate prodrugs of d4T-MP, in which the phosphate group is linked to a phenyl group and the alkyl ester of an amino acid was studied in crude CEM cell extracts. Significant...

L. Naesens, D. Cahard, A. Salgado, L. Bidois… in Purine and Pyrimidine Metabolism in Man IX (1998)

Chapter

In Vitro and in Vivo Inhibitory Activity of the Differentiation-Inducing Agent 9-(2-Phosphonylmethoxyethyl)Adenine (Pmea) Against Rat Choriocarcinoma

The acyclic nucleoside phosphonate 9-(2-phosphonylmethoxyethyl)adenine (PMEA) has previously been shown to be a strong inducer of differentiation in several tumor cell lines. We have now investigated the in vitro

S. Hatse, L. Naesens, B. Degrève… in Purine and Pyrimidine Metabolism in Man IX (1998)

Article

Varicella-zoster virus thymidine kinase gene and antiherpetic pyrimidine nucleoside analogues in a combined gene/chemotherapy treatment for cancer

Ten pyrimidine nucleoside analogues, including (E)-5-(2-bromovinyl)-2′-deoxyuridine (BVDU) and closely related analogues, were evaluated for their cytostatic activity against human osteosarcoma cells transfect...

B Degrève, G Andrei, M Izquierdo, J Piette, K Morin, EE Knaus, LI Wiebe… in Gene Therapy (1997)

Article

Patterns of resistance and sensitivity to antiviral compounds of drug-resistant strains of human cytomegalovirus selected in vitro

Drug-resistant human Cytomegalovirus (HCMV) strains were selected in human embryonic lung (HEL) fibroblasts under pressure of the (S)-3-hydroxy-2-phosphonylmethoxypropyl (HPMP) derivatives of cytosine (HPMPC) ...

R. Snoeck, G. Andrei, E. De Clercq in European Journal of Clinical Microbiology … (1996)

Article

Preface

Alessandro Giacomello, G. J. Peters, Staffan Eriksson… in Pharmacy World and Science (1995)

Article

Comparative activity of selected antiviral compounds against clinical isolates of varicella-zoster virus

Sixteen freshly isolated varicella-zoster virus (VZV) strains were evaluated in vitro, in parallel with two reference strains expressing a functional thymidine kinase (TK⁺) (Oka and YS) and two thymidine kinase-d...

G. Andrei, R. Snoeck, D. Reymen, C. Liesnard… in European Journal of Clinical Microbiology … (1995)