Cytotoxicity of Asymmetric Platinum Complexes against L-1210 Cells. Effect of Bulky Substituents

概要

論文の詳細を見る
The asymmetric platinum complexes cis-Pt(LL')Cl_2 (L=NH_3,L'=CH_3NH_2,(CH_3)_2NH, C_2H_5NH_2 and (C_2H_5)NH and LL'=N, N-dimethylethylenediamine), -one of the NH_3 groups of cis-Pt(NH_3)_2Cl_2 was substituted by alkylamine-, were synthesized and their cytotoxic effects have been measured using L-1210 cells. The IC_<50> values of the asymmetric platinum complexes, -being obtained after 24 h exposure of L-1210 cells to the platinum complexes-, are almost comparable to the corresponding value of cis-Pt(NH_3)_2Cl_2. lIn 2 h exposure, however, the IC_<50> values of the platinum complexes were dramatically chaged, i.e., a marked difference was observed between those of L'=RNH_2 and L'=R_2NH. On the other hand, the amounts of platinum taken into the L-1210 cells is little affected by the alkylamino substitution. The results suggest that the bifunctional platinum binding to the target molecule may be responsible for the cytotoxicity.
公益社団法人日本薬学会の論文
1990-10-25