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
2007; Elsevier BV; Volume: 17; Issue: 9 Linguagem: Inglês
10.1016/j.bmcl.2007.02.021
ISSN1464-3405
AutoresMarco Franceschin, Emanuela Pascucci, Antonello Alvino, Danilo D’Ambrosio, Armandodoriano Bianco, Giancarlo Ortaggi, Maria Savino,
Tópico(s)RNA Interference and Gene Delivery
ResumoFour 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 microM concentration, showing a similar efficiency with respect to each other. Molecular modelling studies are presented to try to explain these findings.
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