Please use this identifier to cite or link to this item: https://open.uns.ac.rs/handle/123456789/19332
Title: Chromatographic lipophilicity and pharmacokinetic behavior of some newly synthesized styryl lactonestereoisomers
Authors: Lončar, Davor
Milošević, Nataša 
Vitas, Jasmina 
Karadžić Banjac, Milica 
Jevrić, Lidija 
Benedeković, Goran 
Issue Date: 2017
Publisher: Novi Sad: University of Novi Sad, Faculty of Technology Novi Sad
Journal: Acta Periodica Technologica
Abstract: The RP-HPLC retention constants of several newly synthesized cytotoxic styryl lactone stereoisomers were determined as parameters of their lipophilicity. Stereochemistry of the compounds has an effect on the retention behavior of only tricyclic isomers. For them, the difference in retention and chromatographic lipophilic parameters are significant. The chromatographic lipophilic parameters of all compounds were correlated with a fourteen computer calculated lipophilic parameters, log P, and pharmacokinetic parameters. Significant linear correlations (R2adj>0.90) were obtained between MLog P and affinity for plasma proteins binding. The correrelations for the other pharmacokinetic parameters were improved by introducing some more molecular descriptors. Multiple linear regression analysis suggested that the volume of distribution depended on the lipopholicity and KaHSA (HSA-human serum albumin) and the absorption through membrane and permeability in the jejunum depend on the lipophilicity and hydrogen bond donors. The tested compounds showed a potent to moderate cytotoxic activity toward several human cancer cells and poor permeation through the blood brain barrier.
URI: https://open.uns.ac.rs/handle/123456789/19332
ISSN: 14507188
DOI: 10.2298/APT1748197L
(BISIS)109804
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