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Design and Synthesis of Some New Furan-Based Derivatives and Evaluation of In Vitro Cytotoxic Activity
New furan-based derivatives have been, designed, synthesized, and evaluated for their cytotoxic and tubulin polymerization inhibitory activities. DNA flow cytometric study of pyridine carbohydrazide 4 and N-phenyl triazinone 7 demonstrated G(2)/M phase cell cycle disruptions. Accumulation of cells i...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9024937/ https://www.ncbi.nlm.nih.gov/pubmed/35458804 http://dx.doi.org/10.3390/molecules27082606 |
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author | Bukhari, Syed Nasir Abbas Ejaz, Hasan Elsherif, Mervat A. Junaid, Kashaf Zaki, Islam Masoud, Reham E. |
author_facet | Bukhari, Syed Nasir Abbas Ejaz, Hasan Elsherif, Mervat A. Junaid, Kashaf Zaki, Islam Masoud, Reham E. |
author_sort | Bukhari, Syed Nasir Abbas |
collection | PubMed |
description | New furan-based derivatives have been, designed, synthesized, and evaluated for their cytotoxic and tubulin polymerization inhibitory activities. DNA flow cytometric study of pyridine carbohydrazide 4 and N-phenyl triazinone 7 demonstrated G(2)/M phase cell cycle disruptions. Accumulation of cells in the pre-G1 phase and positive annexin V/PI staining, which may be caused by degeneration or fragmentation of the genetic components, suggested that cell death occurs via an apoptotic cascade. Furthermore, compounds 4 and 7 had a strong pro-apoptotic impact through inducing the intrinsic mitochondrial mechanism of apoptosis. This mechanistic route was verified by an ELISA experiment that indicated a considerable rise in the levels of p53 and Bax and a drop in the level of Bcl-2 when compared with the control. |
format | Online Article Text |
id | pubmed-9024937 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-90249372022-04-23 Design and Synthesis of Some New Furan-Based Derivatives and Evaluation of In Vitro Cytotoxic Activity Bukhari, Syed Nasir Abbas Ejaz, Hasan Elsherif, Mervat A. Junaid, Kashaf Zaki, Islam Masoud, Reham E. Molecules Article New furan-based derivatives have been, designed, synthesized, and evaluated for their cytotoxic and tubulin polymerization inhibitory activities. DNA flow cytometric study of pyridine carbohydrazide 4 and N-phenyl triazinone 7 demonstrated G(2)/M phase cell cycle disruptions. Accumulation of cells in the pre-G1 phase and positive annexin V/PI staining, which may be caused by degeneration or fragmentation of the genetic components, suggested that cell death occurs via an apoptotic cascade. Furthermore, compounds 4 and 7 had a strong pro-apoptotic impact through inducing the intrinsic mitochondrial mechanism of apoptosis. This mechanistic route was verified by an ELISA experiment that indicated a considerable rise in the levels of p53 and Bax and a drop in the level of Bcl-2 when compared with the control. MDPI 2022-04-18 /pmc/articles/PMC9024937/ /pubmed/35458804 http://dx.doi.org/10.3390/molecules27082606 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Bukhari, Syed Nasir Abbas Ejaz, Hasan Elsherif, Mervat A. Junaid, Kashaf Zaki, Islam Masoud, Reham E. Design and Synthesis of Some New Furan-Based Derivatives and Evaluation of In Vitro Cytotoxic Activity |
title | Design and Synthesis of Some New Furan-Based Derivatives and Evaluation of In Vitro Cytotoxic Activity |
title_full | Design and Synthesis of Some New Furan-Based Derivatives and Evaluation of In Vitro Cytotoxic Activity |
title_fullStr | Design and Synthesis of Some New Furan-Based Derivatives and Evaluation of In Vitro Cytotoxic Activity |
title_full_unstemmed | Design and Synthesis of Some New Furan-Based Derivatives and Evaluation of In Vitro Cytotoxic Activity |
title_short | Design and Synthesis of Some New Furan-Based Derivatives and Evaluation of In Vitro Cytotoxic Activity |
title_sort | design and synthesis of some new furan-based derivatives and evaluation of in vitro cytotoxic activity |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9024937/ https://www.ncbi.nlm.nih.gov/pubmed/35458804 http://dx.doi.org/10.3390/molecules27082606 |
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