Synthesis of Aza-Amanitins to Enhance Cytotoxicity for Targeted Cancer Therapeutics

The development of cancer therapies in which cancer-specific agents can be used to deliver a cytotoxic agent to cancer cells is at the forefront of drug research 1,2 There has been more research into antibody drug conjugates (ADCs) as a method of targeted cancer therapy 3 -amanitin, a highly selective inhibitor of RNA polymerase II (Pol II), produced by the death-cap mushroom targets tumors in a cellcycle independent manner 4 -amanitin as a drug payload for ADCs enhances therapeutic potential and specificity AbstractFigure 1.General reaction scheme to access aza-amanitin analogs.