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吲哚衍生物作为激酶抑制剂在癌症治疗中的最新进展。

Recent Updates on Indole Derivatives as Kinase Inhibitors in the Treatment of Cancer.

机构信息

Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga, Punjab, India.

Gupta College of Technological Sciences, Ashram More, G.T. Road, Asansol, W.B, India.

出版信息

Anticancer Agents Med Chem. 2023;23(4):404-416. doi: 10.2174/1871520622666220607143040.

Abstract

Cancer is becoming a global threat as its treatment accounts for many challenges. Hence, newer inventions prioritize the requirement of developing novel anticancer agents. In this context, kinases have been exclusively investigated and developed as a promising and novel class of drug targets for anticancer regimen. Indole derivatives have been found to be most effective for targeting multiple kinases, such as PIM, CDK, TK, AKT, SRC, PI3K, PKD, GSK, etc., to inhibit cell proliferation for cancer. Recently, a group of researchers have proposed their research outcomes related to this moiety, such as Zhang et al. described some potent PI3K inhibitors by substitution at the 4th position of the indole ring. Kassis et al. enumerated several potent CDK5 inhibitors by substituting the 2nd and 6th positions of the indole ring. In the present review, we have taken the initiative to summarize structure-activity relationship (SAR) studies of indole derivatives as kinase inhibitors for the development of potential inhibitors.

摘要

癌症作为一种全球威胁,其治疗存在诸多挑战。因此,新型发明侧重于开发新型抗癌药物。在这种情况下,激酶已被专门研究和开发为一种有前途的新型药物靶点,用于抗癌方案。吲哚衍生物已被发现对靶向多种激酶(如 PIM、CDK、TK、AKT、SRC、PI3K、PKD、GSK 等)非常有效,可抑制癌细胞增殖。最近,一组研究人员提出了与这部分相关的研究结果,例如 Zhang 等人通过取代吲哚环的第 4 位描述了一些有效的 PI3K 抑制剂。Kassis 等人通过取代吲哚环的第 2 位和第 6 位列举了几种有效的 CDK5 抑制剂。在本综述中,我们主动总结了作为激酶抑制剂的吲哚衍生物的构效关系 (SAR) 研究,以开发潜在的抑制剂。

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