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

Year 2017, Volume: 21 Issue: 4, 949 - 960, 01.12.2017

Bedriye Seda Kurşun-aktar , Emine Elçin Oruç-emre , Ayşegül Karaküçük-iyidoğan Ayse Şahin Yağlıoğlu İbrahim Demirtaş Şaban Tekin

Abstract

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.

Keywords

Chalcone; antiproliferative activity; cytotoxic; morpholine

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