Human telomerase inhibition by substituted acridine derivatives

A series of 3,6-disubstituted acridine derivatives have been rationally des igned as telomerase inhibitors. They have been designed on the basis that i nhibition of telomerase occurs by stabilising G-quadruplex structures forme d by the folding of telomeric DNA. The most potent inhibitors have IC50 val ues against telomerase of between 1.3 and 8 mu M, comparable to their cytot oxicity in ovarian cancer cell lines. (C) 1999 Elsevier Science Ltd. All ri ghts reserved.