English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Tools annual

Global: Zendy Free Plan

Global: Zendy Tools monthly

Global: Zendy Plus monthly

Picoplatin is a sterically hindered antitumor compound with unique chemical and DNA binding properties, but its curative effect is not as good as other platinum drugs. Therefore, a series of sterically hindered fluorine-containing platinum(II) complexes  Y1 – Y5  were synthesized and characterized by introducing fluorine atoms at the 2-position of the pyridine group and different leaving group ligands.  In vitro  antiproliferative activity assessments of these complexes have been performed against A549, MCF-7, SW480, HCT116, HepG2 human cancer cell lines, and LO2 normal cells. The results showed that  Y1  with 2-fluoropyridine coordination and chloride ion as the leaving group exhibited stronger antiproliferative activity and selectivity in the tested cancer cell lines, especially for A549 cancer cells. DNA binding constants were determined by UV absorption and fluorescence titration, and the binding ability of  Y1  to DNA is much stronger than that of the others, which shows  Y1  has better DNA damage ability. For the determination of apoptosis by the complex, the results were consistent with those of the MTT assay, and the apoptosis rate of  Y1  reached 38.9%. Therefore, our work offers an advantageous method for the development of new platinum-based antitumor drugs.

Synthesis, characterization, and biological activity of sterically hindered fluorine-containing platinum(II) complexes