MK2抑制剂氨基噻吩类关键中间体合成路线设计及优化文献综述

 2022-04-14 09:04

MK2抑制剂氨基噻吩类关键中间体的合成与表征

【摘要】:p38 / MAPK激活的激酶2(MK2)途径参与一系列病理例如炎症疾病和转移以及肿瘤的抵抗机制。由于使用p38抑制剂出现了严重的副作用,p38抑制剂都没有进入高级临床试验,出于这个原因,MK2被确定为阻止这种情况的替代目标途径。因此,尽管在开发MK2抑制剂期间遇到了重大困难,MK2仍被认为是治疗炎症和相关疾病的有吸引力的目标,以防止肿瘤转移,并增加肿瘤对化疗药物的敏感性。通过分子库的筛选,选取最优活性的氨基噻吩类化合物进行合成与分析。本论文介绍了MK2抑制剂氨基噻吩类化合物并对其的关键中间体的合成方法进行了综述。

【关键词】丝裂原活化蛋白激酶(MAPK)激活的蛋白激酶2 炎症 结构 功能 现状 信号通路

Synthesis and characterization of key intermediates of aminothiophene as MK2 inhibitor

【Abstract】:The p38 / MAPK activated kinase 2 (MK2) pathway is involved in a series of pathologies such as inflammatory disease and metastasis, as well as tumor resistance mechanisms. Because of the serious side effects of p38 inhibitors, none of p38 inhibitors entered advanced clinical trials. For this reason, MK2 was identified as an alternative target pathway to prevent this situation. Therefore, despite major difficulties encountered during the development of MK2 inhibitors, MK2 is considered an attractive target for the treatment of inflammation and related diseases to prevent tumor metastasis and increase the sensitivity of tumor to chemotherapy drugs. Through the selection of molecular library, the aminothiophene compounds with the best activity were selected for synthesis and analysis.

【Key words】:MK2 ,Inflammation, structure, function, status quo, signaling pathway

目录

1 前言 5

2 简介 5

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