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Synthesis and Evaluation of Heterocycles Based Chalcone Derivatives as Antiproliferative Agents

[ Vol. 18 , Issue. 7 ]

Author(s):

Betül Kaya Çavuşoğlu, Özlem Atlı, Gözde Görmüş, Yusuf Özkay* and Zafer Asım Kaplancıklı   Pages 1044 - 1053 ( 10 )

Abstract:


Background: The lack of selectivity and development of drug-resistance encourage researchers to search for novel, more efficient and multi-targeted agents with less toxicity.

Objective: In this paper, a series of novel chalcone derivatives bearing diverse heterocycles have been synthesized and evaluated for their antiproliferative activity against A549 (human lung adenocarcinoma) and C6 (rat brain glioma) cells.

Method: Structures of the title compounds (3-18) were verified by FT-IR, 1H NMR, 13C NMR, HRMS spectral data and elemental analyses. Antiproliferative activities of the compounds were evaluated using MTT assay, BrdU method, and flow cytometric analysis.

Results: Compounds 9 and 15 were revealed as the most promising cytotoxic agents due to their selectivity towards A549 cells with lower IC50 values (IC50=0.05 μM and IC50=0.0316 μM) than cisplatin (IC50=0.06 μM). Flow cytometric analysis of compounds 9 and 15 showed that they affected lung cancer cells by the apoptotic pathway.

Conclusion: It is concluded that this study will contribute to the research of novel antiproliferative agents.

Keywords:

Chalcone, antiproliferative activity, cytotoxicity, apoptotic pathway, derivatives, heterocycles.

Affiliation:

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskisehir, Anadolu University, Faculty of Pharmacy - Department of Pharmaceutical Toxicology Eskisehir, Anadolu University, Faculty of Pharmacy - Department of Pharmaceutical Toxicology Eskisehir, Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry Eskisehir, Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 26470 Eskisehir



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