Review Article

3-吲哚啉-2-1衍生物作为癌症治疗的激酶抑制剂的发展

卷 29, 期 11, 2022

发表于: 31 August, 2021

页: [1891 - 1919] 页: 29

弟呕挨: 10.2174/0929867328666210831142311

价格: $65

摘要

激酶通过直接或间接地调节癌基因的表达和抗原基因的转录,是肿瘤发生和转移的关键调控因子。相应地,多种3-吲哚啉-2-1衍生物作为癌症治疗的选择性激酶抑制剂,表现出低纳摩尔活性,具有显著的疗效、优越的反应率和令人钦佩的耐受性。特别是,某些3-吲哚啉-2-1衍生物已经满足了临床试验或药物市场的要求。在此,我们关注了3-吲哚啉-2-1衍生物作为癌症治疗激酶抑制剂的特点,概述了3-吲哚啉-2-1衍生物作为癌症治疗激酶抑制剂的最新进展,分析了酪氨酸激酶抑制剂和丝氨酸/丝氨酸/苏氨酸激酶抑制剂的选择性,总结了作为选择性激酶抑制剂的构效关系(SARs),并为3-吲哚啉-2-1衍生物作为癌症治疗激酶抑制剂的开发提供了前景。

关键词: 3-吲哚啉-2-1,激酶抑制剂,构效关系,癌症治疗,恶性肿瘤,ATP结合。

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