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
Descripción
Sumario: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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