A New Naphthopyran Derivative Combines -Myb Inhibition, Microtubule-Targeting Effects, and Antiangiogenic Properties.

Based on the promising -Myb inhibitor , a series of 2-amino-4-aryl-4-naphtho[1,2-]pyran-3-carbonitriles (, -, -) were repurposed or newly synthesized via a three-component reaction of 1-naphthol, and various aryl aldehydes and malononitrile and screened for their -Myb inhibitory activities. also served as a lead compound for seven new naphthopyran derivatives (-), which were cytotoxic with nanomolar IC values, to inhibit the polymerization of tubulin, and to destabilize microtubules in living cells. Especially, the alkyne , originally made for intracellular localization studies using click chemistry, showed an overall high activity in all assays performed.