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标题：In vitro mechanistic investigation of polycyclic cage-like heterocyclic hybrid possessing diverse pharmacophoric units
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作者：Raju Suresh Kumar ; Abdulrahman I. Almansour ; Natarajan Arumugam 等
期刊名称：Journal of King Saud University - Science
印刷版ISSN：1018-3647
出版年度：2020
卷号：32
期号：4
页码：2406-2413
DOI：10.1016/j.jksus.2020.03.029
语种：English
出版社：Elsevier
摘要：AbstractA 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 forin vitroanticancer 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.
关键词：Anticancer activity;Broad spectrum activity;[3 + 2] Cycloaddition;Annulation;Polycyclic cage-like heterocyclic hybrid