In:
Acta Periodica Technologica, National Library of Serbia, , No. 48 ( 2017), p. 197-209
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 (R2 adj〉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 Ka HSA
(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.
Type of Medium:
Online Resource
ISSN:
1450-7188
,
2406-095X
Language:
English
Publisher:
National Library of Serbia
Publication Date:
2017
detail.hit.zdb_id:
2865275-7
