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. © 2007 Elsevier Ltd. All rights reserved.
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 / Marco, Franceschin; Emanuela, Pascucci; Alvino, Antonello; Danilo, D'Ambrosio; Bianco, Armandodoriano; Ortaggi, Giancarlo; Savino, Maria. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 17:9(2007), pp. 2515-2522. [10.1016/j.bmcl.2007.02.021]