MAP3K5抑制剂司隆色替的结构修饰及构效关系研究进展
Advances in Structure Modification and Structure-activity Relationships of MAP3K5 Inhibitor Selonsertib
兰萍萍 1王辉 1刘华 1王甜甜 2王增涛1
作者信息
- 1. 江西中医药大学药学院,江西南昌 330004
- 2. 江西中医药大学中药固体制剂制造技术国家工程研究中心,江西南昌 330006
- 折叠
摘要
作为首个进入临床阶段的有丝分裂原活化蛋白激酶激酶激酶5(MAP3K5)抑制剂,司隆色替临床试验的适用证包括非酒精性脂肪肝、肺动脉高压和糖尿病肾病等.由于司隆色替结构新颖、独特,已成为该类抑制剂结构设计、骨架修饰的主要先导化合物.近年来,围绕司隆色替的结构修饰,获得了大量"me-too"类候选物.文章从骨架片段修饰和成环结构修饰2方面介绍了司隆色替的修饰策略及构效关系的研究进展,旨在为该领域的研究提供参考.
Abstract
As the first mitogen-activated protein kinase kinase kinase 5(MAP3K5)inhibitor in the clinical stage,indications of selonsertib in clinical trials included non-alcoholic steatohepatitis,pulmonary arterial hypertension and diabetic kidney disease.Due to its novel and unique structure,it has become the main lead compound for structural design and backbone modification of this class of inhibitors.In recent years,a large number of"me-too"candidates had been obtained from selonsertib by the structure modification.This paper introduces the progress of structure modification strategies and structure-activity relationships of selonsertib from two aspects of skeleton fragment modification and cyclization structure modification,aiming to provide a reference for research in this field.
关键词
MAP3K5抑制剂/司隆色替/研究进展/结构修饰Key words
MAP3K5 inhibitor/selonsertib/research progress/structure modification引用本文复制引用
基金项目
国家自然科学基金(22067010)
江西省自然科学基金(20224BAB206117)
江西中医药大学博士启动基金(2021BSZR024)
出版年
2024
NETL
NSTL
万方数据