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J Med Chem. 2012 Nov 26;55(22):9785-92. doi: 10.1021/jm301019w. Epub 2012 Oct 18.

Shooting for selective druglike G-quadruplex binders: evidence for telomeric DNA damage and tumor cell death.

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Dipartimento di Scienze Ambientali, Seconda Università di Napoli , 81100 Caserta, Italy.


Targeting of DNA secondary structures, such as G-quadruplexes, is now considered an appealing opportunity for drug intervention in anticancer therapy. So far, efforts made in the discovery of chemotypes able to target G-quadruplexes mainly succeeded in the identification of a number of polyaromatic compounds featuring end-stacking binding properties. Against this general trend, we were persuaded that the G-quadruplex grooves can recognize molecular entities with better drug-like and selectivity properties. From this idea, a set of small molecules was identified and the structural features responsible for G-quadruplex recognition were delineated. These compounds were demonstrated to have enhanced affinity and selectivity for the G-quadruplex over the duplex structure. Their ability to induce selective DNA damage at telomeric level and to induction of apoptosis and senescence on tumor cells is herein experimentally proven.

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