新的噻唑喹啉衍生物2、3a-d、4a-c、5、6a-c和7a、b已被合成。所有制备的化合物均通过MTT细胞毒性测定评估其对三种人类肿瘤细胞系的细胞毒性。化合物3c、3d、4c、6a、6b和7b表现出强力的抗癌活性，几乎与多柔比星相当或更优。表现出显著细胞毒性的化合物进一步被选择研究其对Topo II酶的抑制活性。化合物4c是最有效的Topo II抑制剂，其IC50值为0.23 ± 0.01 µM，比依托泊苷和多柔比星的IC50值高1.4倍和3.6倍。此外，与对照组相比，化合物4c显示出对A549细胞的细胞周期紊乱和凋亡的显著影响。最活跃的化合物的分子对接显示其适当地适配于Topo II活性位点，表明我们设计的化合物是作为Topo II抑制剂发挥有效抗癌功效的有希望的候选药物。

New thiazolopyrimidine derivatives 2, 3a-d, 4a-c, 5, 6a-c, and 7a,b were synthesised. All prepared compounds were evaluated by MTT cytotoxicity assay against three human tumour cell lines. Compounds 3c, 3d, 4c, 6a, 6b, and 7b 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 4c was the most potent Topo II inhibitor with an IC50 value of 0.23 ± 0.01 µM, which was 1.4-fold and 3.6-fold higher than the IC50 values of Etoposide and Doxorubicin. Furthermore, compound 4c 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.