Synthesis and evaluation of potent (iso)ellipticine-based inhibitors of MYLK4 accessed expeditious synthesis from isoquinolin-5-ol.

The KSO-mediated generation of -iminoquinone contributed to the regioselective substitution of isoquinolin-5,8-dione. This hydroxyl group-guided substitution was also applied to selected heterocycles and addressed the regioselectivity issue of quinones. This study has provided an expeditious pathway from isoquinolin-5-ol (5) to ellipticine (1) and isoellipticine (2), which benefits the comprehensive comparison of their activity.