Synthesis of novel bis‐ and poly(benzimidazoles) as well as bis‐ and poly(benzothiazoles) as anticancer agents,Journal of Heterocyclic Chemistry

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Synthesis of novel bis‐ and poly(benzimidazoles) as well as bis‐ and poly(benzothiazoles) as anticancer agents
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-03-07 , DOI: 10.1002/jhet.3947
Ali M. S. Hebishy ₁ , Mohamed S. Abdelfattah ₁ , Abdullah Elmorsy ₁ , Ahmed H. M. Elwahy ₂

Affiliation

A synthesis of bis‐ and poly(benzimidazoles) as well as bis‐ and poly(benzothiazoles) was attempted using different protocols. The best results were obtained by employing the reaction of the appropriate bis‐ or poly(aldehydes) with o‐phenylenediamine or 2‐aminothiophenol, respectively, in ethanol at reflux in the presence of NaHSO₃. The anticancer activities of the synthesized compounds were evaluated against human breast adenocarcinoma cell line (MCF‐7), liver cancer cell line (HepG‐2), and epithelial colorectal adenocarcinoma cells (CaCO‐2). Hexakis(benzothiazole) was found to exhibit the highest activity against HepG‐2 and MCF‐7 cell lines with IC₅₀ values of 21.16 and 13.25 μM, respectively.

中文翻译：

新型双和聚苯并咪唑类以及双和聚苯并噻唑类化合物的合成

尝试使用不同的方案合成双和聚苯并咪唑以及双和聚苯并噻唑。通过在NaHSO ₃存在下，在乙醇中回流使适当的双醛或多醛分别与邻苯二胺或2-氨基硫酚反应，可获得最佳结果。评估了合成化合物对人乳腺癌细胞系（MCF-7），肝癌细胞系（HepG-2）和上皮结直肠腺癌细胞（CaCO-2）的抗癌活性。已发现Hexakis（苯并噻唑）对HepG-2和MCF-7细胞系的活性最高，IC ₅₀值分别为21.16和13.25μM。

更新日期：2020-04-22

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