title: Differential contribution of metal complexation and dimerization to the chemotherapeutic potential of bicyclen-Zn2II complex against human immunodeficiency virus.
abstract: 1,1'-(m-Xylenediyl)-bis(1,4,7,10-tetraazacyclododecane)-Z n2II complex (m-xylenediyl-bicyclin-Zn2II), a potent inhibitor of human immunodeficiency virus (HIV), was obtained from cyclin 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-bicyclin-Zn2II by respectively increasing the CC50 and decreasing the EC50 in comparison with those of cyclin.
authors.affiliation: Institute of Pharmaceutical Sciences, Hiroshima University School of Medicine, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Inouye
authors.forename: T
authors.initials: T
authors.lastname: Kanamori
authors.forename: T
authors.initials: T
authors.lastname: Yoshida
authors.forename: T
authors.initials: T
authors.lastname: Koike
authors.forename: M
authors.initials: M
authors.lastname: Shionoya
authors.forename: H
authors.initials: H
authors.lastname: Fujioka
authors.forename: E
authors.initials: E
authors.lastname: Kimura
mesh_terms: D000998:Antiviral Agents / Q000737:chemistry* / Q000494:pharmacology*; D002478:Cells, Cultured; D000080027:Cyclams; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D005029:Ethylenediamines / Q000737:chemistry* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects*; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D019065:Virus Assembly / Q000187:drug effects
chemical_list: C101432:1,1'-(3-xylenediyl)-bis(1,4,7,10-tetraazacyclodecane); D000998:Antiviral Agents; D000080027:Cyclams; D005029:Ethylenediamines; D006571:Heterocyclic Compounds; C038072:cyclen