Synthesis of 3-hydroxy-2-phenyl-1,8-naphthyridin-4(1H)-one derivatives

Abstract

As part of our research program directed towards the design and synthesis of novel heterocycles with potential cytotoxic activity, we synthesized some 2-phenyl-3-hydroxy-1,8-naphthyridin-4(1H)-one derivatives, structurally related to the antimitotic 2-phenyl-1,8-naphthyridin-4(1H)-ones. To the best of our knowledge, this is the first example of preparation of 3-hydroxy derivatives from the 1,8-napththyridine nucleus. A preliminary cytotoxic evaluation of two of these compounds is also included.