New thiazolopyrimidine derivatives and were synthesised. All prepared compounds were evaluated by MTT cytotoxicity assay against three human tumour cell lines. Compounds and exhibited potent to strong anticancer activity that was nearly comparable or superior to Doxorubicin. Compounds exhibiting significant cytotoxicity were further selected to study their inhibitory activity on the Topo II enzyme. Compound was the most potent Topo II inhibitor with an IC value of 0.23 ± 0.01 µM, which was 1.4-fold and 3.6-fold higher than the IC values of Etoposide and Doxorubicin. Furthermore, compound showed significant cell cycle disruption and apoptosis on A549 cells compared to control cells. Molecular docking of the most active compounds illustrated proper fitting to the Topo II active site, suggesting that our designed compounds are promising candidates for the development of effective anticancer agents acting through Topo II inhibition.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9930781 | PMC |
| http://dx.doi.org/10.1080/14756366.2023.2175209 | DOI Listing |
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