Synthesis and structure-activity relationship study: Anticancer chalcones derived from 4'-morpholinoacetophenone

The aim of this research was to synthesize chalcone derivatives containing morpholine ring and to investigate their antiproliferative activity. The 3-aryl-1-[4-(morpholin- 4-yl)phenyl]prop-2-en-1-one derivatives were synthesized and evaluated for their in vitro antiproliferative activities on C6 cells (Rat glioma cell line) and HeLa cells (Human cervix adenocarcinoma), using the BrdU ELISA assay. The calculation of ADME properties of new chalcone derivatives was used by topological polar surface area (TPSA), absorption (ABS%) and Lipinski's rules. Most of the compounds exhibited significantly antiproliferative activity on two cell lines. Among the screened compounds, compound 7, 10, 11 and 12 revealed higher antiproliferative activity than cisplatin which was used as reference drug. Compound 11 on HeLa cell and compound 10 on C6 cell line are the most effective compared with cisplatin.