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首页> 外文期刊>Current drug research reviews. >Repurposing of Benzimidazole Scaffolds for HER2 Positive Breast Cancer Therapy: An In-Silico Approach
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Repurposing of Benzimidazole Scaffolds for HER2 Positive Breast Cancer Therapy: An In-Silico Approach

机译：再利用HER2的苯并咪唑支架阳性乳腺癌治疗:一个In-Silico方法

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Background: A newer trend has been seen recently to reuse the conventional drugs with distinct indications for the newer applications to speed up the drug discovery and development based on earlier records and safety data. Most of the non-cancerous agents could afford a little or tolerable side effects in individuals. However, the repositioning of these non-cancerous agents for successful anticancer therapy is an outstanding strategy for future anti-cancer drug development. Since more diverse and selective cancer drug targets are being discovered and developed, the approved drug collections are particularly useful to quickly identify clinically advanced anticancer drugs against those targets.Objective: Antihelminthic drugs such as Mebendazole and Albendazole (Benzimidazole class) have been reported to exhibit cytotoxicity (or anticancer activities) against several types of cancer. Therefore, this study aims to repurpose the benzimidazole scaffold for breast cancer treatment.Methods: In the present study, three hydrazone analogs having a benzimidazole motif in their structural frame were synthesized. Their in-silico binding studies against HER2 receptor (PDB ID: 4LQM) and ADMET studies were carried out using Accelrys drug discovery studio 4.1. Cytotoxicity of the synthesized compounds against HER2 overexpressed MCF-7 cell lines was determined by MTT assay.Results: One of the compounds 2-[2-(2,4-dinitrophenyl)hydrazinylidene]-2,3-dihydro-lH-benzimi-dazole (Ul) has shown good cytotoxicity when compared to the standard Lapatinib, which is a well known HER2 inhibitor.Conclusions: Thus, the designed benzimidazole scaffold might serve as the best leads for treating breast cancer, which is additionally confirmed by performing their docking study via Accelrys discovery studio.
机译：背景:最近看到的一个新趋势重用和独特的传统药物适应症较新的应用程序的速度药物发现和开发基于早些时候记录和安全数据。非代理可以很少或可容忍的副作用在个人。这些非代理的重新定位成功是一种抗癌治疗杰出的战略未来的抗癌药物发展。抗癌药物被发现和目标开发、批准药物集合特别有用的快速识别临床上先进的抗癌药物那些目标。甲苯咪唑、阿苯达唑等(苯并咪唑类)已报告具有细胞毒性(或抗癌活动)对几种类型的癌症。研究旨在重新苯并咪唑支架治疗乳腺癌。目前的研究中,三个腙类似物苯并咪唑基序的结构框架是合成的。针对HER2受体(PDB ID: 4 lqm)和ADMET研究使用Accelrys药物发现studio 4.1。合成化合物对HER2过表达MTT比色MCF-7细胞系是化验。

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