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首页> 外文期刊>Archiv der Pharmazie >New Benzimidazoles and Their Antitumor Effects with Aurora A Kinase and KSP Inhibitory Activities
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New Benzimidazoles and Their Antitumor Effects with Aurora A Kinase and KSP Inhibitory Activities

机译：新苯并咪唑及其对极光激酶和KSP抑制活性的抗肿瘤作用

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摘要

A newly synthesized series of anticancer compounds comprising thiazolo[3,2-a]pyrimidine derivatives 6a-q bearing a benzimidazole moiety was produced via a one-pot reaction of N-(4-(1H-benzo[d]imidazol-2-yl)phenyl)-2-cyanoacetamide 5 with 2-aminothiazole and an appropriate aromatic aldehyde. Compound 7 was obtained via the reaction of 4-(1H-benzo[d]imidazol-2yl)benzenamide 1 with carbon disulphide and methyl iodide in the presence of concentrated aqueous solution of NaOH, then treated with o-phenylenediamine to give N-(4-1H-benzo[d]imidazol-2-yl)phenyl)-1H-benzo[d]imidazol-2-amine 8. The structures of the newly synthesized compounds were confirmed by analytical and spectroscopic measurements (IR, MS, and H-1 NMR). The synthesized products were screened and studied for their in vitro antitumor activity against three human cancer cell lines (namely colorectal cancer cell line HCT116, human liver cancer cell line HepG2, and human ovarian cancer cell line A2780) and their Aurora A kinase and KSP inhibitory activities. All newly synthesized compounds revealed marked results comparable with the standard drug CK0106023. The compounds 6e and 6k of the thiazolopyrimidine derivatives were the most active compounds when tested against the three cell lines in comparison with the standard drug CK0106023, and showed potent dual KSP and Aurora A kinase inhibition.
机译：通过N-（4-（1（H-苯并[d]]咪唑-2-）的一锅反应制备了新合成的一系列抗癌化合物，其包含带有苯并咪唑部分的噻唑并[3,2-a]嘧啶衍生物6a-q。基）苯基）-2-氰基乙酰胺5与2-氨基噻唑和适当的芳族醛。在浓NaOH水溶液的存在下，通过4-（1H-苯并[d]咪唑-2基）苯甲酰胺1与二硫化碳和甲基碘的反应得到化合物7，然后用邻苯二胺处理得到N-（ 4-1H-苯并[d]咪唑-2-基）苯基）-1H-苯并[d]咪唑-2-胺8.通过分析和光谱测量（红外，质谱和质谱）确定新合成的化合物的结构。 1 H NMR）。筛选合成产物并研究其对三种人类癌细胞系（即结直肠癌细胞系HCT116，人类肝癌细胞系HepG2和人类卵巢癌细胞系A2780）及其Aurora A激酶和KSP抑制作用的体外抗肿瘤活性活动。所有新合成的化合物均显示出与标准药物CK0106023相当的显着结果。与标准药物CK0106023相比，针对三种细胞系进行测试时，噻唑并嘧啶衍生物的化合物6e和6k是活性最高的化合物，并显示出有效的双重KSP和Aurora A激酶抑制作用。

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