New highly hydrosoluble and not self-aggregated perylene derivatives with three and four polar side-chains as G-quadruplex telomere targeting agents and telomerase inhibitors

Four new perylene derivatives with three and four basic side chains, readily soluble in water and not self-aggregated, are presented here. All four compounds are able to inhibit human telomerase and to induce different G-quadruplex structures. Four new perylene derivatives with three and four basic side-chains are reported here as G-quadruplex interactive compounds. The new perylene derivatives are readily soluble in water and not self-aggregated, in contrast to what happens with the previously reported two side-chain perylene derivatives. All four compounds are able to induce the G-quadruplex and to inhibit 50% of telomerase activity at about 5 μM concentration, showing a similar efficiency with respect to each other. Molecular modelling studies are presented to try to explain these findings.