Acetylenyl substituted nucleic bases and their triphenylphosphonium (TPP) conjugates. Unexpected surge in cytotoxicity

Olga V. Andreeva,Alexandra D. Voloshina,Anna P. Lyubina,Bulat F. Garifullin,Anastasiia S. Sapunova,Syumbelya K. Amerhanova,Irina Yu. Strobykina,Mayya G. Belenok,Olga B. Babaeva,Liliya F. Saifina,Vyacheslav E. Semenov,Vladimir E. Kataev

BIOORGANIC CHEMISTRY（2024）

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摘要

•Acetylenation of nucleobases gave them moderate cytotoxicity against cancer cells.•TPP-conjugates of acetylenated nucleobases exhibited IC50 values of 0.1–0.2 µM.•The selectivity index values reached 120–150.•Induction of apoptosis proceeding along the mitochondrial pathway.•The arrest of the cell cycle in the G0/G1 phase.

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