WATER-SOLUBLE CORONENE DERIVATIVES ACTIVE AS INHIBITORS OF HUMAN TELOMERASE BY INDUCTION OF G-QUADRUPLEX STRUCTURES AND THEIR USE AS ANTICANCER AGENTS

摘要

The coronene derivatives of general formula: (I); wherein R1, R2, R2', R3, R4 and R4', when present and different from H, represent hydrophilic chains, constitute a new family of compounds that can selectively induce the formation of G-quadruplex structures in the telomeric DNA, and can thus act as inhibitors of the telomerase enzyme, thereby inhibiting tumour proliferation. These compounds proved to have a strong anticancer activity in vitro, which was assessed with many human tumour cell lines. Preparations including the coronene derivatives of formula (I) as active ingredients are proposed as medicament for use in anticancer treatments.