| Literature DB >> 6682656 |
B Salles, J L Butour, C Lesca, J P Macquet.
Abstract
A comparison of the inhibition of DNA synthesis by the two geometrical bidentate isomers cis- and trans-Pt(NH3)2Cl2 and by the monodentate [Pt(dien)Cl]Cl in a model used for screening potential antitumor compounds, the L1210 leukemia cells, is presented. The efficacy of penetration after a 2 hours Pt treatment is in the order trans (8) greater than cis (1) approximately dien (0.7). DNA replication is reduced to 50% of the control when 1.8 X 10(-4), 2.4 X 10(-4) and 80 X 10(-4) Pt atoms were bound per nucleotide for cis, trans and dien derivatives, respectively. If we admit that DNA is the pharmacological target of Pt antitumor compounds, these results suggest that a quantitative inhibition of DNA synthesis is certainly not correlated with antitumor activity.Entities:
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Year: 1983 PMID： 6682656 DOI： 10.1016/0006-291x(83)91500-0
Source DB: PubMed Journal: Biochem Biophys Res Commun ISSN： 0006-291X Impact factor: 3.575