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Merck

Caspase dependent apoptotic activity of polycyclic cage-like heterocyclic hybrids.

Saudi journal of biological sciences (2020-12-12)
Raju Suresh Kumar, Abdulrahman I Almansour, Natarajan Arumugam, D Kotresha, Janardhana Papayya Balakrishna
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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 12.14ย ยฑย 1.53 and 10.68ย ยฑย 0.68ย ยตM, 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.

MATERIALS
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Camptothecin, phyproofยฎ Reference Substance
Sigma-Aldrich
1,3-Propylene sulfite, 99%
Sigma-Aldrich
(S)-(+)-Camptothecin, โ‰ฅ90% (HPLC), powder