AI Article Synopsis
- The study investigates four olivacine derivatives to determine which has the strongest antitumor activity against cancer cell lines CCRF/CEM and MCF-7.
- The testing included several methods such as comet assays and molecular docking to evaluate how each compound interacts with DNA and topoisomerase II.
- Among the compounds, one (9-methoxy-5,6-dimethyl-1-({[1-hydroxy-2-(hydroxymethyl)butan-2-yl]amino}methyl)-6-pyrido[4,3-]carbazole) showed the best potential as an anticancer drug due to its high affinity for topoisomerase II and minimal genotoxic effects.
Article Abstract
Olivacine and ellipticine are model anticancer drugs acting as topoisomerase II inhibitors. Here, we present investigations performed on four olivacine derivatives in light of their antitumor activity. The aim of this study was to identify the best antitumor compound among the four tested olivacine derivatives. The study was performed using CCRF/CEM and MCF-7 cell lines. Comet assay, polarography, inhibition of topoisomerase II activity, histone acetylation, and molecular docking studies were performed. Each tested compound displayed interaction with DNA and topoisomerase II, but did not cause histone acetylation. Compound (9-methoxy-5,6-dimethyl-1-({[1-hydroxy-2-(hydroxymethyl)butan-2-yl]amino}methyl)-6-pyrido[4,3-]carbazole) was found to be the best candidate as an anticancer drug because it had the highest affinity for topoisomerase II and caused the least genotoxic damage in cells.
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8395211 | PMC |
| http://dx.doi.org/10.3390/ijms22168492 | DOI Listing |
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Article Synopsis
- The study investigates four olivacine derivatives to determine which has the strongest antitumor activity against cancer cell lines CCRF/CEM and MCF-7.
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