4.5 Article

Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids

期刊

SAUDI JOURNAL OF BIOLOGICAL SCIENCES
卷 27, 期 12, 页码 3290-3300

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ELSEVIER
DOI: 10.1016/j.sjbs.2020.09.042

关键词

Cage-like heterocyclic hybrids; HCT116; JURKAT; Apoptosis; Cell cycle; TUNEL Assay; Caspase 3

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资金

  1. King Saud University, Riyadh, Saudi Arabia [RSP-2020/231]

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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 IC50 values of compound 1g against HCT116 and JURKAT cell lines are 12.14 +/- 1.53 and 10.68 +/- 0.68 mu M, 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 anticancer agent. (C) 2020 The Author(s). Published by Elsevier B.V. on behalf of King Saud University.

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