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Synthesis and in vitro Anticancer Activity of Novel Heterocycles Utilizing Thiophene Incorporated Thioureido Substituent as Precursors

机译:利用噻吩掺入硫代丙酮取代基的新型杂环的合成和体外抗癌活性作为前体

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摘要

Ethyl 2-(3-allylthioureido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate (1) was used as a building block for synthesis of new heterocycles. Pyrimidine and thiazole moieties were achieved upon condensation of compound 1 with various reagents such as chloroacetic acid, dietyl malonate, ninhydrin, 2,3-epoxy-2,3-dihydro-1,4-naphthoquinone, and hydrazine hydrate. The structures of the newly synthesized compounds were confirmed using spectral measurements. The prepared products were evaluated for their anticancer activity against colon HCT-116 human cancer cell line. Compounds 6, 9, 10a, 11, 12, 15 have displayed potent activity.
机译:将2-(3-烯丙基硫胺)-4,5,6,7-四氢苯并[B]噻吩-3-羧酸盐(1)用作合成新杂环的结构块。 在化合物1用各种试剂如氯乙酸,尿酸亚酮酸,茚三酮,2,3-环氧-2,3-二氢-1,4-萘醌和肼水合物等各种试剂来实现嘧啶和噻唑部分。 使用光谱测量确认新合成化合物的结构。 评估制备的产物对抗结肠HCT-116人癌细胞系的抗癌活性。 化合物6,9,10a,11,12,15显示出有效的活性。

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