Promising Anticancer Drug Candidates Based on the 7-methoxychromone Scaffold: Synthesis and Evaluation of Antiproliferative Activity

18 chromone derivatives were designed and synthesized from paeonol. All synthetic compounds were evaluated for their anti-proliferative activity towards eight human cancer cell lines including HepG2, HL-60, KB, LLC, LNCaP, LU-1, MCF7, and SW480. Compounds 3g and 3h presented the best cytotoxic effects towards tested cancer cell lines except HepG2. Their IC50 values were ranging from 7.9±0.4 to 18.9±1.3 μg/mL. Meanwhile, compound 3l showed selective cytotoxicity against MCF7 and KB with IC50 of 13.7±0.6 and 15.5±0.9 μg/mL, respectively. Keywords: Anti-cancer activity, Imidazolidin-4-one, 7-Methoxychromone, Paeonol, Pyrimidine-2, 4, 6(1H, 3H, 5H)-trione, Semi-synthesis.