Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry
ISSN: 0975-413X
Abstract
Investigation of the spectrum of applicability of quinolineamides
Author(s): Ewelina Spaczyńska, Dominik Tabak, Katarzyna Malarz and Robert MusiolAntiproliferative activity of the synthesized compounds was tested by the MTS assay against the wild type of human colon adenocarcinoma cell line (HCT116) and mutants with disabled TP53 gene (HCT116 p53-/-). The compounds were also tested for their cytotoxicity against murinemelanoma cell line (B16-F10) and normal human dermal fibroblasts(NHDF). One of the studied compounds (3g) was found active inhibiting the proliferation of all tumor cell lines.Moreover, spectroscopic characterization for the quinolines was performed. The cellular localization of two compounds with the highest fluorescence intensity(3e and3h) was also determined. These results suggest the quinoline derivatives accumulate in mitochondria but not penetrate the nuclei of cells. In summary, agroup of quinoline analogues showing good potential as candidates for imaging agents. The most active compound being superior to standarddoxorubicine is interesting leading structure for further modification.
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Citations : 15261
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