Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids

A small library of cage-like heterocyclic hybrids encompassing pyrroloisoquinolines, pyridinone and acenaphthene structural moieties have been synthesized and tested for their potential as anticancer agents against HCT116 and JURKAT cell lines. The results revealed that these cell lines are more sen...

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Detalles Bibliográficos
Autores principales: Kumar, Raju Suresh, Almansour, Abdulrahman I., Arumugam, Natarajan, Kotresha, D., Balakrishna, Janardhana Papayya
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2020
Materias:
Original Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7715051/
https://www.ncbi.nlm.nih.gov/pubmed/33304134
http://dx.doi.org/10.1016/j.sjbs.2020.09.042
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author Kumar, Raju Suresh
Almansour, Abdulrahman I.
Arumugam, Natarajan
Kotresha, D.
Balakrishna, Janardhana Papayya
author_facet Kumar, Raju Suresh
Almansour, Abdulrahman I.
Arumugam, Natarajan
Kotresha, D.
Balakrishna, Janardhana Papayya
author_sort Kumar, Raju Suresh
collection PubMed
description A small library of cage-like heterocyclic hybrids encompassing pyrroloisoquinolines, pyridinone and acenaphthene structural moieties have been synthesized and tested for their potential as anticancer agents against HCT116 and JURKAT cell lines. The results revealed that these cell lines are more sensitive towards compound 1g and it showed dose dependent cytotoxic effect at 48 hrs of incubation. The IC(50) values of compound 1g against HCT116 and JURKAT cell lines are 12.14 ± 1.53 and 10.68 ± 0.68 µM, respectively. Further studies on the determination of mechanism of action of compound 1g discovered that it brought the cell death by inducing Caspase 3 dependent apoptosis and also by arresting the cell cycle at S phase. These studies revealed that compound 1g can be recommended as a potential anti-cancer agent.
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spelling pubmed-77150512020-12-09 Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids Kumar, Raju Suresh Almansour, Abdulrahman I. Arumugam, Natarajan Kotresha, D. Balakrishna, Janardhana Papayya Saudi J Biol Sci Original Article A small library of cage-like heterocyclic hybrids encompassing pyrroloisoquinolines, pyridinone and acenaphthene structural moieties have been synthesized and tested for their potential as anticancer agents against HCT116 and JURKAT cell lines. The results revealed that these cell lines are more sensitive towards compound 1g and it showed dose dependent cytotoxic effect at 48 hrs of incubation. The IC(50) values of compound 1g against HCT116 and JURKAT cell lines are 12.14 ± 1.53 and 10.68 ± 0.68 µM, respectively. Further studies on the determination of mechanism of action of compound 1g discovered that it brought the cell death by inducing Caspase 3 dependent apoptosis and also by arresting the cell cycle at S phase. These studies revealed that compound 1g can be recommended as a potential anti-cancer agent. Elsevier 2020-12 2020-09-25 /pmc/articles/PMC7715051/ /pubmed/33304134 http://dx.doi.org/10.1016/j.sjbs.2020.09.042 Text en © 2020 The Author(s) http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Original Article
Kumar, Raju Suresh
Almansour, Abdulrahman I.
Arumugam, Natarajan
Kotresha, D.
Balakrishna, Janardhana Papayya
Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
title Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
title_full Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
title_fullStr Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
title_full_unstemmed Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
title_short Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
title_sort caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7715051/
https://www.ncbi.nlm.nih.gov/pubmed/33304134
http://dx.doi.org/10.1016/j.sjbs.2020.09.042
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