Design, synthesis and biological evaluation of ß-boswellic acid based HDAC inhibitors as inducers of cancer cell death.

The synthesis and bio-evaluation of naturally occurring boswellic acids (BAs) as an alternate CAP for the design of new HDAC inhibitors is described. All the compounds were screened against a panel of human cancer cell lines to identify leads, which were subsequently examined for their potential to inhibit HDACs. The identified lead compound showed IC50 value of 6µm for HDACs, found to induce G1 cell cycle arrest at significantly low concentration (1µM) and caused significant loss in mitochondrial membrane potential at 5 and 10µM. Furthermore, specific interactions of the lead molecule inside the catalytic domain were also studied through in silico molecular modeling.