Synthesis and biological activity of squaramido-tethered bisbenzimidazoles as synthetic anion transporters,RSC Advances

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Synthesis and biological activity of squaramido-tethered bisbenzimidazoles as synthetic anion transporters
RSC Advances ( IF 3.9 ) Pub Date : 2021-1-20 , DOI: 10.1039/d0ra10189c
Zhong-Kun Wang ₁ , Xiao-Qiao Hong ₂ , Jinhui Hu ₁ , Yuan-Yuan Xing ₁ , Wen-Hua Chen _{1,

3}

Affiliation

A series of squaramido-tethered bisbenzimidazoles were synthesized from the reaction of diethyl squarate with substituted 2-aminomethylbenzimidazoles. These conjugates exhibit moderate binding affinity toward chloride anions. They are able to facilitate the transmembrane transport of chloride anions most probably via an anion exchange process, and tend to be more active at acidic pH than at physiological pH. The viability of these conjugates toward four selected solid tumor cell lines was evaluated using an MTT assay and the results suggest that some of these conjugates exhibit moderate cytotoxicity probably in an apoptotic fashion.

中文翻译：

方酰胺基双苯并咪唑作为合成阴离子转运体的合成及其生物活性

由方酸二乙酯与取代的 2-氨基甲基苯并咪唑反应合成一系列方酰胺基双苯并咪唑。这些缀合物对氯阴离子表现出中等的结合亲和力。它们最有可能通过阴离子交换过程促进氯阴离子的跨膜转运，并且在酸性 pH 值下比在生理 pH 值下更活跃。使用 MTT 测定评估这些缀合物对四种选定实体肿瘤细胞系的活力，结果表明这些缀合物中的一些可能以凋亡方式表现出中度细胞毒性。

更新日期：2021-01-20

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