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标题：Diastereoselective synthesis and anticancer potential of a small library of cage-like heterocyclic hybrids
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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：2021
卷号：33
期号：1
页码：1-8
DOI：10.1016/j.jksus.2020.101238
语种：English
出版社：Elsevier
摘要：Graphical abstractPolycyclic cage-like heterocyclic hybrids comprising structurally diverse heterocyclic units have been synthesized in good yields. Anticancer evaluation of these compounds against MCF-7 and NCI-H460 cell lines revealed dose dependent reduction with significant anticancer activity. Compound4binhibited these cell lines respectively with IC50of 10.86 ± 0.94 and 9.17 ± 0.63 µM. Apoptosis and cell cycle analysis in MCF-7 revealed that this compound was able to induce early apoptosis.Display OmittedAbstractWith an aim to construct novel anticancer drugs, a series of polycyclic heterocycles comprising diverse structural sub-units based on molecular hybridization strategy have been designed and synthesized through a three-component [3 + 2]-cycloaddition/annulation strategy. Anticancer evaluation of these compounds against MCF-7 and NCI-H460 cell lines revealed dose dependent reduction with noteworthy anticancer activity. Compound4binhibited MCF-7 and NCI-H460 cell lines with IC50values 10.86 ± 0.94 and 9.17 ± 0.63 µM respectively. Further, apoptosis and cell cycle analysis revealed that this compound was able to prompt apoptosis at an early stage in MCF-7 cell line besides increasing the threshold of MMP and % of cells expressing FITC-dUTP. These results suggest that compound4bis a potential molecule for the further exploration.
关键词：Cage-like heterocyclic hybrids;Stereoselective synthesis;MCF-7;Flow cytometry;Apoptosis;JC1;Cell cycle;TUNEL assay;Caspase 3