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Synthesis and Cytotoxicity Evaluation of Novel Asymmetrical Mono-Carbonyl Analogs of Curcumin (AMACs) against Vero, HeLa, and MCF7 Cell Lines
A series of novel asymmetrical mono-carbonyl analogs of curcumin (AMACs) were synthesized and evaluated for cytotoxic activity using BSLT and MTT assay against Vero, HeLa, and MCF7 cell lines. The structures of the synthesized compounds were confirmed by FTIR, (1)H-NMR, (13)C-NMR, and mass spectral...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6027665/ https://www.ncbi.nlm.nih.gov/pubmed/29880783 http://dx.doi.org/10.3390/scipharm86020025 |
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author | Wiji Prasetyaningrum, Pekik Bahtiar, Anton Hayun, Hayun |
author_facet | Wiji Prasetyaningrum, Pekik Bahtiar, Anton Hayun, Hayun |
author_sort | Wiji Prasetyaningrum, Pekik |
collection | PubMed |
description | A series of novel asymmetrical mono-carbonyl analogs of curcumin (AMACs) were synthesized and evaluated for cytotoxic activity using BSLT and MTT assay against Vero, HeLa, and MCF7 cell lines. The structures of the synthesized compounds were confirmed by FTIR, (1)H-NMR, (13)C-NMR, and mass spectral data. The results of the cytotoxicity evaluation showed that the synthesized compounds exhibited moderate to very high toxic activity in BSLT (LC(50) value 29.80–1704.23 µM); most of the compound exhibited cytotoxic activity against HeLa cell lines, which is comparable to the activity of cisplatin (IC(50) value 40.65–95.55 µM), and most of the compound tested against MCF7 cell lines exhibited moderate to very high cytotoxic activity (IC(50) value 7.86–35.88 µM). However, the selectivity index (SI) of the compounds was low (<1–1.96). Among the synthesized compounds, compound 1b was the most cytotoxic and selective against MCF7 cell lines. It could be considered for further development to obtain the more active and selective chemotherapeutic agents against breast cancer. |
format | Online Article Text |
id | pubmed-6027665 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-60276652018-07-02 Synthesis and Cytotoxicity Evaluation of Novel Asymmetrical Mono-Carbonyl Analogs of Curcumin (AMACs) against Vero, HeLa, and MCF7 Cell Lines Wiji Prasetyaningrum, Pekik Bahtiar, Anton Hayun, Hayun Sci Pharm Article A series of novel asymmetrical mono-carbonyl analogs of curcumin (AMACs) were synthesized and evaluated for cytotoxic activity using BSLT and MTT assay against Vero, HeLa, and MCF7 cell lines. The structures of the synthesized compounds were confirmed by FTIR, (1)H-NMR, (13)C-NMR, and mass spectral data. The results of the cytotoxicity evaluation showed that the synthesized compounds exhibited moderate to very high toxic activity in BSLT (LC(50) value 29.80–1704.23 µM); most of the compound exhibited cytotoxic activity against HeLa cell lines, which is comparable to the activity of cisplatin (IC(50) value 40.65–95.55 µM), and most of the compound tested against MCF7 cell lines exhibited moderate to very high cytotoxic activity (IC(50) value 7.86–35.88 µM). However, the selectivity index (SI) of the compounds was low (<1–1.96). Among the synthesized compounds, compound 1b was the most cytotoxic and selective against MCF7 cell lines. It could be considered for further development to obtain the more active and selective chemotherapeutic agents against breast cancer. MDPI 2018-06-07 2018 /pmc/articles/PMC6027665/ /pubmed/29880783 http://dx.doi.org/10.3390/scipharm86020025 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Wiji Prasetyaningrum, Pekik Bahtiar, Anton Hayun, Hayun Synthesis and Cytotoxicity Evaluation of Novel Asymmetrical Mono-Carbonyl Analogs of Curcumin (AMACs) against Vero, HeLa, and MCF7 Cell Lines |
title | Synthesis and Cytotoxicity Evaluation of Novel Asymmetrical Mono-Carbonyl Analogs of Curcumin (AMACs) against Vero, HeLa, and MCF7 Cell Lines |
title_full | Synthesis and Cytotoxicity Evaluation of Novel Asymmetrical Mono-Carbonyl Analogs of Curcumin (AMACs) against Vero, HeLa, and MCF7 Cell Lines |
title_fullStr | Synthesis and Cytotoxicity Evaluation of Novel Asymmetrical Mono-Carbonyl Analogs of Curcumin (AMACs) against Vero, HeLa, and MCF7 Cell Lines |
title_full_unstemmed | Synthesis and Cytotoxicity Evaluation of Novel Asymmetrical Mono-Carbonyl Analogs of Curcumin (AMACs) against Vero, HeLa, and MCF7 Cell Lines |
title_short | Synthesis and Cytotoxicity Evaluation of Novel Asymmetrical Mono-Carbonyl Analogs of Curcumin (AMACs) against Vero, HeLa, and MCF7 Cell Lines |
title_sort | synthesis and cytotoxicity evaluation of novel asymmetrical mono-carbonyl analogs of curcumin (amacs) against vero, hela, and mcf7 cell lines |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6027665/ https://www.ncbi.nlm.nih.gov/pubmed/29880783 http://dx.doi.org/10.3390/scipharm86020025 |
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