Stiff-stilbene ligands target G-quadruplex DNA and exhibit selective anticancer and antiparasitic activity

March 25, 2020

Well done to Mike (again ;-)), Pablo and Rosina, who was an final year project student in our group, for their latest paper on the synthesis,  biophysical characterization and in vitro screening of a series of stiff-stilbene G4 binding ligands featuring differing electronics, side-chain chemistries and molecular geometries. The ligands display selectivity for G4 DNA over duplex DNA and exhibit nanomolar toxicity against Trypasanoma brucei and HeLa cancer cells whist remaining up to two orders of magnitude less toxic to non-tumoral mammalian cell line MRC5. Our study demonstrates that stiff-stilbenes show exciting potential as the basis of selective anticancer and antiparasitic therapies.

 

 

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