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Differential Contribution of Metal Complexation and Dimerization to the Chemotherapeutic Potential of Bicyclen-ZnI2I Complex against Human Immunodeficiency Virus
- Source :
- Biological and Pharmaceutical Bulletin. 19:456-458
- Publication Year :
- 1996
- Publisher :
- Pharmaceutical Society of Japan, 1996.
-
Abstract
- 1, 1'-(m-Xylenediyl)-bis (1, 4, 7, 10-tetraazacyclododecane)-ZnII2 complex (m-xylenediyl-bicyclen-ZnII2), a potent inhibitor of human immunodeficiency virus (HIV), was obtained from cyclen by a combination of dimerization and metal complexation. The ratio of median cytotoxic concentration against host cells (CC50) and median effective concentration against HIV cytopathogenicity (EC50), referred to as the selectivity index (SI), was regarded to be a measure of anti-HIV activity. These two chemical modifications contributed to a potent, in vitro anti-HIV activity of m-xylenediyl-bicyclen-ZnII2 by respectively increasing the CC50 and decreasing the EC50 in comparison with those of cyclen.
- Subjects :
- Pharmacology
Stereochemistry
Virus Assembly
Pharmaceutical Science
General Medicine
Cyclams
Ethylenediamines
Antiviral Agents
In vitro
Virus
chemistry.chemical_compound
Cytopathogenic Effect, Viral
chemistry
Cyclen
Heterocyclic Compounds
Cell culture
HIV-1
Humans
Cytotoxic T cell
Polyamine
Selectivity
Cells, Cultured
EC50
Subjects
Details
- ISSN :
- 13475215 and 09186158
- Volume :
- 19
- Database :
- OpenAIRE
- Journal :
- Biological and Pharmaceutical Bulletin
- Accession number :
- edsair.doi.dedup.....c529e316ceb82baed8b75ee3753d8e0a