Diversity Oriented Synthesis of Benzoxanthene and Benzochromene Libraries via One-Pot, Three-Component Reactions and Their Anti-proliferative Activity

Abstract

Libraries of benzoxanthenes, as well as of benzochromenes, were efficiently synthesized via one-pot, three-component reactions of 2-naphthol, aldehydes, and cyclic 1,3-diketones/malononitrile/ethyl cyanoacetate in the presence of catalytic amount of ceric ammonium nitrate (CAN) under solvent free conditions. The protocol offers rapid synthesis of structurally diverse benzoxanthenes and benzochromenes for biologically screening. All the synthesized compounds were evaluated for their anti-proliferative activity, and several compounds were exhibiting promising anti-proliferative activity.