Differential Contribution of Metal Complexation and Dimerization to the Chemotherapeutic Potential of Bicyclen-Zn^II₂ Complex against Human Immunodeficiency Virus

抄録

1, 1'-(m-Xylenediyl)-bis (1, 4, 7, 10-tetraazacyclododecane)-Zn^II₂ complex (m-xylenediyl-bicyclen-Zn^II₂), 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-Zn^II₂ by respectively increasing the CC₅₀ and decreasing the EC₅₀ in comparison with those of cyclen.