Publication in Journal of Photochemistry and Photobiology B: Biology

In this paper, we described the preparation and thorough characterization of a series of platinum(II) iodido complexes of the general formula cis-[PtI2(Ln)2], where Ln stands for O-substituted 9-deazahypoxanthine derivatives. The complexes exhibited significant wide-spectrum anticancer activity in vitro against ten human cell lines (MCF7, HOS, A549, HeLa, G-361, 22Rv1, PC-3, HepG2, A2780 and A2780R), with IC50 ≈ 0.5–24.0 μM. Very good correlation between the lipophilicity parameter logP and IC50 values of anticancer activity in vitro were obtained by simple QSAR analysis. The in vivo testing of the representative complexes 1, 4 and 5 on a L1210 leukemia model revealed their positive effect on the prolongation of the mean survival time. The 1H NMR and ESI-MS interaction studies revealed the ability of complexes to interact with selected biomolecules and enabled us to describe some molecular mechanisms of these interactions and hydrolytic activation of the prepared compounds.

 

 

 

 

Date: 14. jun 2017 | Author: agch

Department of Inorganic Chemistry

Faculty of Science
Palacký University in Olomouc

17. listopadu 12
CZ-771 46 Olomouc
Czech Republic

tel: +420 585 634 351
fax: +420 585 634 357
email : agch(at)upol.cz