New calix[4]arene conjugates that present polycyclic aro-matic hydrocarbons (PAHs) at their exo rims have been syn-thesized by esterification of a cone-shaped calix[4]arene-dicarboxylic acid with trans-orcis-pyrenylisoxazolidinylalcohols prepared by a 1,3-dipolar cycloaddition methodol-ogy. The in vitro cytotoxic activities of all compounds were evaluated with three different human tumor cell lines, andthe most potent one reached an IC50of 95 nM. The differentbiological activities of the synthesized compounds were ex-plained by docking and circular dichroism studies, which ev-idenced their intercalating abilities from the DNA minorgroove.
DNA Recognition with Polycyclic-Aromatic-Hydrocarbon-Presenting Calixarene Conjugates
RESCIFINA, Antonio;Zagni C;MINEO, PLACIDO;CHIACCHIO, Ugo;
2014-01-01
Abstract
New calix[4]arene conjugates that present polycyclic aro-matic hydrocarbons (PAHs) at their exo rims have been syn-thesized by esterification of a cone-shaped calix[4]arene-dicarboxylic acid with trans-orcis-pyrenylisoxazolidinylalcohols prepared by a 1,3-dipolar cycloaddition methodol-ogy. The in vitro cytotoxic activities of all compounds were evaluated with three different human tumor cell lines, andthe most potent one reached an IC50of 95 nM. The differentbiological activities of the synthesized compounds were ex-plained by docking and circular dichroism studies, which ev-idenced their intercalating abilities from the DNA minorgroove.| File | Dimensione | Formato | |
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