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Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer
In the current work, a new set of carbohydrazide linked benzofuran-isatin conjugates (5a–e and 7a–i) was designed and synthesised. The anticancer activity for compounds (5b–d, 7a, 7b, 7d and 7g) was measured against NCI-55 human cancer cell lines. Compound 5d was the most efficient, and thus subject...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Taylor & Francis
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8245078/ https://www.ncbi.nlm.nih.gov/pubmed/34176414 http://dx.doi.org/10.1080/14756366.2021.1944127 |
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author | Eldehna, Wagdy M. Salem, Rofaida Elsayed, Zainab M. Al-Warhi, Tarfah Knany, Hamada R. Ayyad, Rezk R. Traiki, Thamer Bin Abdulla, Maha-Hamadien Ahmad, Rehan Abdel-Aziz, Hatem A. El-Haggar, Radwan |
author_facet | Eldehna, Wagdy M. Salem, Rofaida Elsayed, Zainab M. Al-Warhi, Tarfah Knany, Hamada R. Ayyad, Rezk R. Traiki, Thamer Bin Abdulla, Maha-Hamadien Ahmad, Rehan Abdel-Aziz, Hatem A. El-Haggar, Radwan |
author_sort | Eldehna, Wagdy M. |
collection | PubMed |
description | In the current work, a new set of carbohydrazide linked benzofuran-isatin conjugates (5a–e and 7a–i) was designed and synthesised. The anticancer activity for compounds (5b–d, 7a, 7b, 7d and 7g) was measured against NCI-55 human cancer cell lines. Compound 5d was the most efficient, and thus subjected to the five-dose screen where it showed excellent broad activity against almost all tested cancer subpanels. Furthermore, all conjugates (5a–e and 7a–i) showed a good anti-proliferative activity towards colorectal cancer SW-620 and HT-29 cell lines, with an excellent inhibitory effect for compounds 5a and 5d (IC(50) = 8.7 and 9.4 µM (5a), and 6.5 and 9.8 µM for (5d), respectively). Both compounds displayed selective cytotoxicity with good safety profile. In addition, both compounds provoked apoptosis in a dose dependent manner in SW-620 cells. Also, they significantly inhibited the anti-apoptotic Bcl2 protein expression and increased the cleaved PARP level that resulted in SW-620 cells apoptosis. |
format | Online Article Text |
id | pubmed-8245078 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Taylor & Francis |
record_format | MEDLINE/PubMed |
spelling | pubmed-82450782021-07-09 Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer Eldehna, Wagdy M. Salem, Rofaida Elsayed, Zainab M. Al-Warhi, Tarfah Knany, Hamada R. Ayyad, Rezk R. Traiki, Thamer Bin Abdulla, Maha-Hamadien Ahmad, Rehan Abdel-Aziz, Hatem A. El-Haggar, Radwan J Enzyme Inhib Med Chem Research Paper In the current work, a new set of carbohydrazide linked benzofuran-isatin conjugates (5a–e and 7a–i) was designed and synthesised. The anticancer activity for compounds (5b–d, 7a, 7b, 7d and 7g) was measured against NCI-55 human cancer cell lines. Compound 5d was the most efficient, and thus subjected to the five-dose screen where it showed excellent broad activity against almost all tested cancer subpanels. Furthermore, all conjugates (5a–e and 7a–i) showed a good anti-proliferative activity towards colorectal cancer SW-620 and HT-29 cell lines, with an excellent inhibitory effect for compounds 5a and 5d (IC(50) = 8.7 and 9.4 µM (5a), and 6.5 and 9.8 µM for (5d), respectively). Both compounds displayed selective cytotoxicity with good safety profile. In addition, both compounds provoked apoptosis in a dose dependent manner in SW-620 cells. Also, they significantly inhibited the anti-apoptotic Bcl2 protein expression and increased the cleaved PARP level that resulted in SW-620 cells apoptosis. Taylor & Francis 2021-06-28 /pmc/articles/PMC8245078/ /pubmed/34176414 http://dx.doi.org/10.1080/14756366.2021.1944127 Text en © 2021 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Paper Eldehna, Wagdy M. Salem, Rofaida Elsayed, Zainab M. Al-Warhi, Tarfah Knany, Hamada R. Ayyad, Rezk R. Traiki, Thamer Bin Abdulla, Maha-Hamadien Ahmad, Rehan Abdel-Aziz, Hatem A. El-Haggar, Radwan Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer |
title | Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer |
title_full | Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer |
title_fullStr | Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer |
title_full_unstemmed | Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer |
title_short | Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer |
title_sort | development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in colon cancer |
topic | Research Paper |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8245078/ https://www.ncbi.nlm.nih.gov/pubmed/34176414 http://dx.doi.org/10.1080/14756366.2021.1944127 |
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