Various fused‐heterocyclic‐derivatives containing thiazolopyridine moieties has been synthesized by allowing 5‐aminothiazolo[3,2‐a]pyridine derivative 1 to undergo annulations reactions with different reagents under different‐reaction conditions. The biological assessment of compounds 2 , 11 , 14 , 15 , and 19 showed remarkable antimicrobial activities. In addition, selected derivatives of the products were screened for their anticancer activities against two tumor cell lines using MTT assay and the results showed that some of these compounds have potent cytotoxic effect, as concluded from their IC₅₀ values. Meanwhile, compounds 3a , 7 have exhibited very strong potency as anticancer candidates. Thiazolopyridine structures have been confirmed as a useful lead compounds for the development of new anticancer agents. Molecular docking showed that,‐some of the synthesized compounds more suitable inhibitor against‐ALR2 with farther alteration in future.

中文翻译：

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噻唑并吡啶合成的各种稠合杂环及其药理和抗菌评价

通过使5-氨基噻唑并[3,2-a]吡啶衍生物1在不同的反应条件下与不同的试剂进行环化反应，已经合成了各种含噻唑并吡啶部分的稠合杂环衍生物。化合物的生物评估2，11，14，15，和19显示出显着的抗微生物活性。另外，使用MTT测定法筛选了产物的选定衍生物对两种肿瘤细胞系的抗癌活性，结果表明，从它们的IC ₅₀值可以得出结论，这些化合物中的一些具有强的细胞毒性作用。同时，化合物3a，7种具有很强的抗癌潜力。噻唑并吡啶结构已被证实是开发新抗癌剂的有用前导化合物。分子对接表明，某些合成的化合物将来更适用于ALR2抑制剂。