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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...

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Autores principales: Bukhari, Syed Nasir Abbas, Ejaz, Hasan, Elsherif, Mervat A., Junaid, Kashaf, Zaki, Islam, Masoud, Reham E.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
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.
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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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