In vitro mechanistic investigation of polycyclic cage-like heterocyclic hybrid possessing diverse pharmacophoric units
| Autor: | Natarajan Arumugam, Abdulrahman I. Almansour, Raju Suresh Kumar |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Annulation
Multidisciplinary Stereochemistry DNA damage Polycyclic cage-like heterocyclic hybrid 02 engineering and technology 010501 environmental sciences 021001 nanoscience & nanotechnology 01 natural sciences Jurkat cells Anticancer activity In vitro chemistry.chemical_compound chemistry Cell culture Broad spectrum activity Moiety MTT assay lcsh:Science (General) 0210 nano-technology [3 + 2] Cycloaddition DNA lcsh:Q1-390 0105 earth and related environmental sciences |
| Zdroj: | Journal of King Saud University: Science, Vol 32, Iss 4, Pp 2406-2413 (2020) |
| ISSN: | 1018-3647 |
| Popis: | A novel polycyclic cage-like heterocyclic hybrid comprising several privileged structures such as pyrroloisoquinoline, 4-pyridinone and a α,β -unsaturated ketone moiety has been synthesized in good yield employing a microwave mediated [3 + 2]-cycloaddition/annulation strategy in 1-butyl-3-methylimidazolium bromide ([bmim]Br). The compound thus synthesized was analyzed for in vitro anticancer activity employing MCF-7, Jurkat, HCT 116 and NCI-H460 cell lines. The effect of polycyclic cage-like heterocyclic hybrid on cells viability was analyzed by MTT assay and its DNA damage efficiency was confirmed by several examinations like apoptosis study, cell cycle analysis, caspase-3 expression analysis and TUNEL assay. Mitochondrial membrane potential was determined by JC-1 staining. The polycyclic cage-like heterocyclic hybrid bearing diverse functionalities played a major role in DNA damage of cancerous cells and in consequence inhibited the DNA cells proliferation. |
| Databáze: | OpenAIRE |
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