2‐Aminothiophene 3 was achieved through the one‐pot multicomponent reaction of cycloheptanone, cyanoacetamide, elemental sulfur, and morpholine in ethanol. Diazotization of 2‐aminothiophene 3 with NaNO₂/HCl gave the corresponding diazonium salt 4 , that combined with the appropriate active methylene components; 5a , 5b , 7 , 11 , 13 , 16 , 18 , 21 , 9 , 19 , 22a , and 22b in pyridine (AcONa/EtOH) to form the corresponding hydrazones 6a , 6b , 8 , 10 , 14 , 15 , 17 , 20 , 23 , 24 , 25a , and 25b , respectively. Heating of compound 8 with malononitrile 9 in ethanol gave the thiazole 10 . Treatment of compound 10 , 25a , and 25b with hydrazine hydrate achieve the pyrazoles 12 , 27a , and 27b , respectively. Hydrazinolysis of compound 14 with hydrazine hydrate, followed by condensation of the obtained hydrazide 15 with acetylacetone 19 gave the pyrazole 20 . The recently orchestrated thiophenes were assessed for their cytotoxic action. The result revealed that compound 12 indicated comparable and better action towards HePG2, HCT‐116, MCF‐7, and PC3 cancer cell lines than Doxorubicin.

中文翻译：

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某些带有吡唑部分的新型环庚[b]噻吩-3-羧酰胺的合成及体外抗癌活性

2-氨基噻吩3是通过环庚酮，氰基乙酰胺，元素硫和吗啉在乙醇中的单锅多组分反应制得的。用NaNO ₂ / HCl将2-氨基噻吩3重氮化，得到相应的重氮盐4，并与适当的活性亚甲基组分合并；图5a，图5b，7，11，13，16，18，21，9，19，22A，和22B中在吡啶（AcONa / EtOH）中以形成相应的腙图6a，6b中，8，10，14，15，17，20，23，24，25A，和25B，分别。将化合物8与丙二腈9在乙醇中加热，得到噻唑10。化合物的治疗10，25A，和25B与水合肼实现吡唑12，27A，和图27b。将化合物14与水合肼水合肼解，然后将所得酰肼15与乙酰丙酮19缩合，得到吡唑20。评估最近精心策划的噻吩的细胞毒性作用。结果表明，化合物12对阿霉素，HCT‐116，MCF‐7和PC3癌细胞的作用与阿霉素相当且更好。