29 Result(s)

Article

2-aminothiophene-3-carboxylic acid ester derivatives as novel highly selective cytostatic agents

Cytostatic agents often do not discriminate in their cytostatic potential between different tumor cell types in vitro. In this study, several 2-aminothiophene-3-carboxylic acid ester derivatives were discovere...

J. Balzarini, J. Thomas, S. Liekens, S. Noppen, W. Dehaen… in Investigational New Drugs (2014)

Article

Synthesis and Anti-HIV-1 Activity of 1-[ω-(Phenoxy)Alkyl and -Alkenyl]Uracil Derivatives

1-[ω-(Phenoxy)alkyl and -alkenyl]uracil derivatives were synthesized via condensation of equimolar amounts of 2,4-bis(trimethylsilyloxy)pyrimidine and 1-halo-ω-(phenoxy)alkane or -alkene in order to discover new ...

M. P. Paramonova, D. A. Babkov, V. T. Valuev-Elliston… in Pharmaceutical Chemistry Journal (2013)

Article

Enhanced toxicity of purine nucleoside analogs in cells expressing Drosophila melanogaster nucleoside kinase mutants

The multisubstrate deoxyribonucleoside kinase of Drosophila melanogaster (Dm-dNK) is investigated for possible use as a suicide gene in combined gene/chemotherapy of cancer. The enzyme has broader substrate speci...

N Solaroli, M Johansson, J Balzarini, A Karlsson in Gene Therapy (2007)

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

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)

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

Preface

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

Chapter

Anti-Retroviral and Pharmacological Properties of 9-(2-Phosphonylmethoxyethyl)Adenine (PMEA)

Acyclic nucleoside phosphonates (ANP) represent a structural class of compounds that contain a phosphonate group linked to an acyclic (alkyl) side chain of purine or pyrimidine bases.^1-3 Due to the unusual direct...

J. Balzarini in Purine and Pyrimidine Metabolism in Man VIII (1994)

Article

Key lectures

J. Balzarini, M. Gross, T. Kulikowski, G. J. Peters… in Pharmacy World and Science (1993)

Article

Abstracts of oral presentations

R. Boulieu, A. Lenoir, J. F. Mornex, C. Bohman, J. Balzarini… in Pharmacy World and Science (1993)