基于1H-吡唑并[3,4-b]吡啶母核PI3Kδ抑制剂的设计合成  

Design and Synthesis of PI3Kδ Inhibitor Based on 1H-Pyrazolo[3,4- b ]pyridine Structure

作　　者：田宇奇 兰明 王强[1] 郑永胜 TIAN Yuqi;LAN Ming;WANG Qiang;ZHENG Yongsheng(School of Pharmaceutical Sciences,South-Central Minzu University,Wuhan 430074,China)

机构地区：[1]中南民族大学药学院,湖北武汉430074

出　　处：《洛阳理工学院学报（自然科学版）》2024年第2期1-9,共9页Journal of Luoyang Institute of Science and Technology：Natural Science Edition

基　　金：国家自然科学基金项目(81073208).

摘　　要：恶性肿瘤严重危害人类健康与生命,磷脂酰肌醇-3激酶家族(PI3Ks)在细胞增殖、分化过程中起着重要作用,该激酶及其相关通路的其他激酶可被药物干预,是抗癌药物的热门靶点。在以往的PI3K抑制剂中,均有1H-吡唑并[3,4-b]吡啶母核,通过虚拟筛选以及合成路线设计,合成了一系列1H-吡唑并[3,4-b]吡啶类化合物,该类化合物可能对PI3Kδ具有潜在抑制作用。Malignant tumours pose a significant threat to human health and life.The Phosphatidylinositol 3-kinase(PI3Ks)family plays a pivotal role in cell proliferation and differentiation.This kinase and other kinases associated with its pathway can be targeted by pharmaceutical interventions,making them a popular target for anti-cancer drugs.Among previous PI3K inhibitors,a common 1H-pyrazolo[3,4-b]pyridine structure was identified.Through virtual screening and synthetic route design,a series of 1H-pyrazolo[3,4-b]pyridine compounds were synthesized,which may potentially inhibit PI3Kδ.

关 键 词：PI3K抑制剂 有机合成 1H-吡唑并[3 4-b]吡啶 抗癌药 

分 类 号：O621.3[理学—有机化学] R914.5[理学—化学]