Synthesis and Cytotoxic Activity of New Chalcones and their Flavonol Derivatives
Received Date: Nov 14, 2017 / Accepted Date: Nov 20, 2017 / Published Date: Nov 25, 2017
A series of chalcones and respective flavonols have been synthesized to explore their anti-cancer activities. All the chalcones were synthesized by the reaction between aldehydes and substituted acetophenones in typical base carried Claisen-Schmidt condensation and their corresponding flavonols were synthesized by hydrogen peroxide oxidized Flynn-Algar-Oymada epoxidation and cyclization. The synthesized compounds were characterized by FTIR, 1H NMR, 13C NMR and Mass spectrometry and subjected for cytotoxicity test on MCF-7, HT-29 and HeLa cell lines. Maximum number of compounds demonstrated anti-proliferative activity with IC50 in the range of 18.67-174.3 μM. Compound 3h with a chloro group and 1-phenyl-3(4-methoxy phenyl)-4-pyrazolyl moiety and the flavonol 4a with 3-thienyl group were found to be most potent compounds among all the tested compounds against MCF-7 cell lines with IC50 18.67 and 23.79 μM respectively. The most active compound 3h also showed high docking score of -8.825.
Keywords: Chalcone; Flavonol; Anti-proliferative activity
Citation: Kotha RR, Kulkarni RG, Garige AK, Nerella SG, Garlapati A (2017) Synthesis and Cytotoxic Activity of New Chalcones and their Flavonol Derivatives. Med Chem (Los Angeles) 7:353-360. Doi: 10.4172/2161-0444.1000480
Copyright: © 2017 Kotha RR, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
Select your language of interest to view the total content in your interested language
Share This Article
- Total views: 2286
- [From(publication date): 0-2017 - Dec 09, 2019]
- Breakdown by view type
- HTML page views: 2144
- PDF downloads: 142