alexa Synthesis and Cytotoxic Activity of New Chalcones and their Flavonol Derivatives | OMICS International| Abstract
ISSN: 2161-0444

Medicinal Chemistry
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  • Research Article   
  • Med chem (Los Angeles) 2017, Vol 7(11): 353
  • DOI: 10.4172/2161-0444.1000480

Synthesis and Cytotoxic Activity of New Chalcones and their Flavonol Derivatives

Rathnakar Reddy Kotha1*, Ravindra G Kulkarni2, Anil Kumar Garige1, Sridhar Goud Nerella3 and Achaiah Garlapati1*
1University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Telangana, India
2SVERI’s College of Pharmacy, , Pandhapur, Maharashtra, India
3Molecular Modeling Facility, Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, , Hyderabad, Telangana, India
*Corresponding Author (s) : Rathnakar Reddy Kotha, University College of Pharmaceutical Sciences, Kakatiya University, Warangal-506 009, Telangana, India, Tel: +919949314355, Email: [email protected]
Achaiah Garlapati, University College of Pharmaceutical Sciences, Kakatiya University, Warangal-506 009, Telangana, India, Tel: +919440601057, Email: [email protected]

Received Date: Nov 14, 2017 / Accepted Date: Nov 20, 2017 / Published Date: Nov 25, 2017

Abstract

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.

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