Cytotoxicity of asymmetric platinum complexes against L-1210 cells. Effect of bulky substituents.

Abstract:

:The asymmetric platinum complexes cis-Pt(LL')Cl2 (L = NH3, L' = CH3NH2, (CH3)2NH, C2H5NH2 and (C2H5)2NH and LL' = N,N-dimethylethylenediamine),--one of the NH3 groups of cis-Pt(NH3)2Cl2 was substituted by alkylamine--, were synthesized and their cytotoxic effects have been measured using L-1210 cells. The IC50 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(NH3)2Cl2. In 2 h exposure, however, the IC50 values of the platinum complexes were dramatically changed, i.e., a marked difference was observed between those of L' = RNH2 and L' = R2NH. 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.

authors

Hirano T,Inagaki K,Fukai T,Alink M,Nakahara H,Kidani Y

doi

10.1248/cpb.38.2850

subject

Has Abstract

pub_date

1990-10-01 00:00:00

pages

2850-2

issue

10

eissn

0009-2363

issn

1347-5223

journal_volume

38

pub_type

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