2020 EJRNL PP Oindrila Biswas - 1.pdf
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Terbatas Irwan Sofiyan
» ITB
Terbatas Irwan Sofiyan
» ITB
Small-molecule-based Cl? ion carriers are gaining revived attention
because of their recently discovered role toward anticancer activity. Herein, we
showed that the anticancer agents, PITENINs, have an efficient transmembrane
Cl? ion transport activity. Theoretical calculations, 1H NMR titration, and
spectrophotometric analysis suggest that the PITENINs strongly bind with a Cl?
ion. In addition to the lipophilicity, the presence of both acylthiourea and phenolic
OH moieties of the compounds plays a crucial role in the transport of Cl? ions.
Among the tested compounds, PIT-1 and DM-PIT-1 showed higher Cl? ion
selectivity and transport efficiency. Mechanistic studies demonstrated that the
potent compounds follow the H+/Cl? transport pathway. Cellular activity studies
showed that the disruption of Cl? ion homeostasis by PIT-1 and DM-PIT-1
preferentially promotes apoptotic cell death.