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Searching for new cytotoxic agents based on chromen-4-one and chromane-2,4-dione scaffolds
Cancer is a major cause of death worldwide and novel anticancer agents for its better management are much needed. Benzopyrone-based compounds, such as chromones, possess several distinctive chemical and biological properties, of which the cytotoxicity against cancer cells seems to be prominent. In t...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Medknow Publications & Media Pvt Ltd
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6407335/ https://www.ncbi.nlm.nih.gov/pubmed/30936935 http://dx.doi.org/10.4103/1735-5362.251855 |
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author | Gaspar, Alexandra Mohabbati, Maryam Cagide, Fernando Razzaghi-Asl, Nima Miri, Ramin Firuzi, Omidreza Borges, Fernanda |
author_facet | Gaspar, Alexandra Mohabbati, Maryam Cagide, Fernando Razzaghi-Asl, Nima Miri, Ramin Firuzi, Omidreza Borges, Fernanda |
author_sort | Gaspar, Alexandra |
collection | PubMed |
description | Cancer is a major cause of death worldwide and novel anticancer agents for its better management are much needed. Benzopyrone-based compounds, such as chromones, possess several distinctive chemical and biological properties, of which the cytotoxicity against cancer cells seems to be prominent. In this study, two series of compounds based on chromen-4-one (3-10) and chromane-2,4-dione (11-18) scaffolds were synthesized in moderate/high yields and evaluated for cytotoxicity against HL-60, MOLT-4, and MCF-7 cancer cells using MTT assay. In general, the compounds exhibited moderate cytotoxic effects against the cancer cell lines, among which, a superior potency could be observed against MOLT-4 cells. Chroman-2,4-dione (11-18) derivatives had overall higher potencies compared to their chromen-4-one (3-10) counterparts. Compound 13 displayed the lowest IC(50) values against HL-60 (IC(50), 42.0 ± 2.7 μM) and MOLT-4 cell lines (IC(50), 24.4 ± 2.6 μM), while derivative 11 showed the highest activity against MCF-7 cells (IC(50), 68.4 ± 3.9 μM). In conclusion, this study provides important information on the cytotoxic effects of chromone derivatives. Benzochroman-2,4-dione has been identified as a promising scaffold, which its potency can be modulated by tailored synthesis with the aim of finding novel and dissimilar anticancer compounds. |
format | Online Article Text |
id | pubmed-6407335 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | Medknow Publications & Media Pvt Ltd |
record_format | MEDLINE/PubMed |
spelling | pubmed-64073352019-04-01 Searching for new cytotoxic agents based on chromen-4-one and chromane-2,4-dione scaffolds Gaspar, Alexandra Mohabbati, Maryam Cagide, Fernando Razzaghi-Asl, Nima Miri, Ramin Firuzi, Omidreza Borges, Fernanda Res Pharm Sci Original Article Cancer is a major cause of death worldwide and novel anticancer agents for its better management are much needed. Benzopyrone-based compounds, such as chromones, possess several distinctive chemical and biological properties, of which the cytotoxicity against cancer cells seems to be prominent. In this study, two series of compounds based on chromen-4-one (3-10) and chromane-2,4-dione (11-18) scaffolds were synthesized in moderate/high yields and evaluated for cytotoxicity against HL-60, MOLT-4, and MCF-7 cancer cells using MTT assay. In general, the compounds exhibited moderate cytotoxic effects against the cancer cell lines, among which, a superior potency could be observed against MOLT-4 cells. Chroman-2,4-dione (11-18) derivatives had overall higher potencies compared to their chromen-4-one (3-10) counterparts. Compound 13 displayed the lowest IC(50) values against HL-60 (IC(50), 42.0 ± 2.7 μM) and MOLT-4 cell lines (IC(50), 24.4 ± 2.6 μM), while derivative 11 showed the highest activity against MCF-7 cells (IC(50), 68.4 ± 3.9 μM). In conclusion, this study provides important information on the cytotoxic effects of chromone derivatives. Benzochroman-2,4-dione has been identified as a promising scaffold, which its potency can be modulated by tailored synthesis with the aim of finding novel and dissimilar anticancer compounds. Medknow Publications & Media Pvt Ltd 2019-02 /pmc/articles/PMC6407335/ /pubmed/30936935 http://dx.doi.org/10.4103/1735-5362.251855 Text en Copyright: © 2019 Research in Pharmaceutical Sciences http://creativecommons.org/licenses/by-nc-sa/4.0 This is an open access journal, and articles are distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as appropriate credit is given and the new creations are licensed under the identical terms. |
spellingShingle | Original Article Gaspar, Alexandra Mohabbati, Maryam Cagide, Fernando Razzaghi-Asl, Nima Miri, Ramin Firuzi, Omidreza Borges, Fernanda Searching for new cytotoxic agents based on chromen-4-one and chromane-2,4-dione scaffolds |
title | Searching for new cytotoxic agents based on chromen-4-one and chromane-2,4-dione scaffolds |
title_full | Searching for new cytotoxic agents based on chromen-4-one and chromane-2,4-dione scaffolds |
title_fullStr | Searching for new cytotoxic agents based on chromen-4-one and chromane-2,4-dione scaffolds |
title_full_unstemmed | Searching for new cytotoxic agents based on chromen-4-one and chromane-2,4-dione scaffolds |
title_short | Searching for new cytotoxic agents based on chromen-4-one and chromane-2,4-dione scaffolds |
title_sort | searching for new cytotoxic agents based on chromen-4-one and chromane-2,4-dione scaffolds |
topic | Original Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6407335/ https://www.ncbi.nlm.nih.gov/pubmed/30936935 http://dx.doi.org/10.4103/1735-5362.251855 |
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