Relationships between the chromatographic retention data and the effects of nucleoside derivatives in highly metastatic 3LL cells

G. Pogány, T. Cserháti, J. Oláh, K. Valkó

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

The effect of 21 nucleoside derivatives on the [3H]-thymidine cellular uptake and on the incorporation into DNA of highly metastatic 3LL (Lewis lung carcinoma) cells has been measured. Hydrophobic and hydrophilic molecular parameters (the adsorption capacity, specific adsorption surface, lipophilicity and specific hydrophobic surface area) have been determined by using thin-layer chromatography. Stepwise linear regression analysis and principal component analysis have been applied in order to reveal the relationships between the molecular parameters and the effect of the nucleoside derivatives on highly metastatic 3LL cells. The first principal component obtained from the measured activity data could be attributed to the change of [3H]-thymidine cellular uptake caused by the nucleoside, while the second principal component could be regarded as the measure of the effect on the DNA incorporation of[3 H]-thymidine. The effect of the nucleosides on the [3H]-thymidine uptake could be explained by the specific hydrophobic and adsorption surface area of the nucleoside, on the other hand the effect on the DNA incorporation could be described by the adsorption characteristics (specific hydrophilic surface area and adsorption capacity) of the derivatives.

Original languageEnglish
Pages (from-to)495-500
Number of pages6
JournalJournal of Pharmaceutical and Biomedical Analysis
Volume10
Issue number7
DOIs
Publication statusPublished - Jul 1992

Keywords

  • Lewis lung carcinoma
  • Nucleoside derivatives
  • chromatographic retention parameters
  • hydrophobicity.
  • quantitative structure-activity relationships

ASJC Scopus subject areas

  • Analytical Chemistry
  • Pharmaceutical Science
  • Drug Discovery
  • Spectroscopy
  • Clinical Biochemistry

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