Synthesis and evaluation of the antitumor activity of polyhalo acridone derivatives

Abstract

A series of polyhalo acridone heterocyclic compounds were synthesized and evaluated for their in vitro antitumor activity. It was noteworthy that halogen atoms were present at the 1, 3 and 4 sites of the compounds, and an amide group or a cyano group was at the 2 site. The antitumor bioactivity screening revealed that all the compounds exhibited potent antitumor activity. In particular, compounds 4d, 4o, 5j and 5k showed good antineoplastic selectivity, with a survival rate above 50% in NIH3T3 mouse embryonic cells. The IC₅₀ values were 8.69–13.06 μM in A431 cells. A preliminary assessment of the structure–selectivity relationship of the compounds was also performed.