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  • Title: Synthesis and Enantiomeric Separation of a Novel Spiroketal Derivative: A Potent Human Telomerase Inhibitor with High in Vitro Anticancer Activity.
    Author: Fuggetta MP, De Mico A, Cottarelli A, Morelli F, Zonfrillo M, Ulgheri F, Peluso P, Mannu A, Deligia F, Marchetti M, Roviello G, Reyes Romero A, Dömling A, Spanu P.
    Journal: J Med Chem; 2016 Oct 13; 59(19):9140-9149. PubMed ID: 27592503.
    Abstract:
    The synthesis, the enantiomeric separation, and the characterization of new simple spiroketal derivatives have been performed. The synthesized compounds have shown a very high anticancer activity. Cell proliferation assay showed that they induce a remarkable inhibition of cell proliferation in all cell lines treated, depending on culture time and concentration. The compounds have also shown a potent nanomolar human telomerase inhibition activity and apoptosis induction. CD melting experiments demonstrate that spiroketal does not affect the G-quadruplex (G4) thermal stability. Docking studies showed that telomerase inhibition could be determined by a spiroketal interaction with the telomerase enzyme.
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