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.
Anti-Cancer Agents in Medicinal Chemistry
Title:Synthesis and Evaluation of Heterocycles Based Chalcone Derivatives as Antiproliferative Agents
Volume: 18 Issue: 7
Author(s): Betül Kaya Çavuşoğlu, Özlem Atlı, Gözde Görmüş, Yusuf Özkay*Zafer Asım Kaplancıklı
Affiliation:
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskisehir,Turkey
Keywords: Chalcone, antiproliferative activity, cytotoxicity, apoptotic pathway, derivatives, heterocycles.
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.
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Cite this article as:
Çavuşoğlu Kaya Betül , Atlı Özlem , Görmüş Gözde , Özkay Yusuf *, Kaplancıklı Asım Zafer , Synthesis and Evaluation of Heterocycles Based Chalcone Derivatives as Antiproliferative Agents, Anti-Cancer Agents in Medicinal Chemistry 2018; 18 (7) . https://dx.doi.org/10.2174/1871520618666180105163657
DOI https://dx.doi.org/10.2174/1871520618666180105163657 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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