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首页> 外文期刊>RSC Advances >Design, synthesis and biological evaluation of novel amide-linked 18β-glycyrrhetinic acid derivatives as novel ALK inhibitors
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Design, synthesis and biological evaluation of novel amide-linked 18β-glycyrrhetinic acid derivatives as novel ALK inhibitors

机译：新型酰胺连接的18β-甘草酸衍生物的设计，合成及生物学评价为新的ALK抑制剂

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A series of novel amide-linked 18β-glycyrrhetinic acid derivatives were developed by incorporating substituted piperazine amide fragments into the C30–COOH of 18β-glycyrrhetinic acid scaffold. The synthesized compounds were evaluated for their anticancer activity against Karpas299, A549, HepG2, MCF-7, and PC-3 cell lines by MTT assay. Besides, some compounds with electron-withdrawing groups on phenyl moieties exhibited noticeable antiproliferative activity. The most potent compound 4a was also found to be non-toxic to normal human hepatocytes LO2 cells. The compound 4a exhibited moderate inhibitory activity against wild-type ALK with an IC _(50) value of 203.56 nM and relatively weak potent activity to c-Met (IC _(50) > 1000 nM). Molecular docking studies were performed to explore the diversification in bonding patterns between the compound 4a and Crizotinib.
机译：通过将取代的哌嗪酰胺片段掺入18β-甘草酸支架的C30-COOH中，开发了一系列新的酰胺连接的18β-甘草酸衍生物。通过MTT测定评估对karpas299，a549，hepg2，MCF-7和PC-3细胞系的抗癌活性的合成化合物。此外，一些具有苯基部分的吸电子基团的化合物表现出明显的抗增殖活性。还发现最有效的化合物4a对正常人肝细胞LO2细胞无毒。化合物4A对野生型Alk的中等抑制活性具有203.56nm的IC _（50）值，并且相对较弱的有效活性至C-Met（IC _（50）> 1000nm）。进行分子对接研究以探讨化合物4a和x序列布之间的粘合图案中的多样化。

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