Synthetic
ion transporters have attracted tremendous attention
for their therapeutic potential against various ion-transport-related
diseases, including cancer. Inspired by the structure and biological
activities of natural products, we synthesized a small series of squaramide
and thiourea derivatives of quinine and investigated their ion transport
activities. The involvement of a quinuclidine moiety for the cooperative
interactions of Cl– and H+ ions with
the thiourea or squaramide moiety resulted in an effectual transport
of these ions across membranes. The interference of ionic equilibrium
by the potent Cl– ion carrier selectively induced
cancer cell death by endorsing caspase-arbitrated apoptosis. In vivo
assessment of the potent ionophore showed an efficient reduction in
tumor growth with negligible immunotoxicity to other organs.
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