Synthesis and Evaluation of Heterocycles Based Chalcone Derivatives as Antiproliferative Agents

Author(s): Betül Kaya Çavuşoğlu, Özlem Atlı, Gözde Görmüş, Yusuf Özkay*, Zafer Asım Kaplancıklı

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 18 , Issue 7 , 2018

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Graphical 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.

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Article Details

Year: 2018
Page: [1044 - 1053]
Pages: 10
DOI: 10.2174/1871520618666180105163657
Price: $65

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