Synthesis of novel quinoline-2-one based chalcones of potential anti-tumor activity

► Novel quinoline-2-one chalcones 16 of potential antitumor activity were obtained. ► Products 16 were obtained via a Claisen-Schmidt condensation. ► Some aldols were isolated as key intermediates in the formation of 16. ► Products were screened by the US (NCI) against 60 different human tumor cell lines. ► Product 27 showed the highest in vitro activity being referred to in vivo assays.