Synthesis of Mono- and Bis-substituted Anthraquinones as Inhibitors of Human Telomerase

A number of anthraquinone derivatives have been synthesized in good yield and tested for their ability to inhibit the enzymes telomerase and Taq polymerase using a modified telomeric repeat amplification protocol. In addition, all the synthesized compounds were screened against a panel of ovarian carcinoma cell lines (A2780, CH1 and SKOV-3) to determine their cytotoxicity. All compounds tested inhibited telomerase at a concentration of 10 μM, but showed negligible inhibition of Taq polymerase. None of the compounds tested displayed significant general cell toxicity in ovarian cancer cell lines. The synthesized compounds are potential selective inhibitors of human telomerase.