The present invention provides hTERT modulators and methods for producing and using the same. In particular, the present invention provide a compound of the formula as described herein. Some aspects of the invention are based on the characterization of the effect of hTERT core promoter region mutants on the 5-12 G-quadruplex structure and its stability. It is believed that some of the compounds of the invention bind selectively to the G-quadruplex in the hTERT core promoter mutant, which results in reversal of the effect of mutant promoter activation.