Background: A wide range of thiazole, pyrazole and pyran derivatives gained special attention due to pharmacological activities especially therapeutic activities. Many pharmacological drugs containing the thiazole and pyrazole nuclei are known in the market.

Methods: The 2-arylidencyclohexan-1,3-dione 3a-c were the key starting compounds for many heterocyclic reactions to produce substituted heterocyclic derivatives.

Results: Antiproliferative activities of the produced compounds against six cancer cell lines A549, HT-29, MKN-45, U87MG, SMMC-7721 and H460 were measured in which the compounds showed high inhibition. The most promising compounds were tested against tyrosine kinases (c-Kit, Flt-3, VEGFR-2, EGFR, and PDGFR). Structure-Activity Relationship (SAR) was rationalized by assessing the varying structural features of the molecules. In addition, the most active compounds were selected for Pim-1 inhibition.

Conclusion: Thirty compounds were synthesized. Ten of them (3a, 3c, 5a, 5c, 7a, 10f, 11a, 13c, 16a and 16c) were the most active compounds for selected cancer cell lines. Compounds 3c, 5c, 7a, 10f, 13c and 16c showed high inhibition toward the tyrosine kinases while compounds 3c, 5c and 10f were the most potent to inhibit Pim-1.

背景：由于其药理活性，尤其是治疗活性，各种噻唑，吡唑和吡喃衍生物得到了特别的关注。市场上已知许多含有噻唑和吡唑核的药理药物。

方法：2-芳基环己基-1,3-二酮3a-c是许多杂环反应生成取代杂环衍生物的关键起始化合物。

结果：测定了所产生的化合物对六种癌细胞系A549，HT-29，MKN-45，U87MG，SMMC-7721和H460的抗增殖活性，其中所述化合物显示出高抑制作用。测试了最有前途的化合物对抗酪氨酸激酶的作用（c-Kit，Flt-3，VEGFR-2，EGFR和PDGFR）。通过评估分子的不同结构特征来合理化结构-活性关系（SAR）。另外，选择最具活性的化合物来抑制Pim-1。

结论：合成了三十种化合物。其中十种（3a，3c，5a，5c，7a，10f，11a，13c，16a和16c）是所选癌细胞系中活性最高的化合物。化合物3c，5c，7a，10f，13c和16c显示出对酪氨酸激酶的高度抑制作用，而化合物3c，5c和10f最有效地抑制了Pim-1。