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3-肼基吲哚啉-2-酮衍生物:作为抗癌剂的化学分类及靶标研究。

3-Hydrazinoindolin-2-one derivatives: Chemical classification and investigation of their targets as anticancer agents.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Egyptian Russian University, Badr City, Cairo 11829, Egypt.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo 11562, Egypt.

出版信息

Eur J Med Chem. 2016 Oct 21;122:366-381. doi: 10.1016/j.ejmech.2016.06.034. Epub 2016 Jun 20.

Abstract

Isatin is a well acknowledged pharmacophore in many clinically approved drugs used for treatment of cancer. 3-Hydrazinoindolin-2-one, as a derivative of isatin, represents a pharmacophore of an important class of biologically active pharmaceutical agents by virtue of their diverse biological activities. In this review, anticancer activity will be on focus for compounds derived from 3-hydrazinoindolin-2-one. They are classified according to their chemical structure into nine different classes. In each class, different compounds were browsed, showing their anticancer activity and their potential targets. Moreover, crystallographic data or docking studies were highlighted for some compounds, when available, to provide a deep understanding of their mechanisms of action.

摘要

靛红是许多已批准用于癌症治疗的临床药物中公认的药效团。3-肼基吲哚啉-2-酮作为靛红的衍生物,因其具有多种生物活性,代表了一类重要的具有生物活性的药物配体。在这篇综述中,将重点介绍源于 3-肼基吲哚啉-2-酮的化合物的抗癌活性。根据其化学结构,将它们分为九类。在每一类中,浏览了不同的化合物,展示了它们的抗癌活性和潜在的靶标。此外,还突出显示了一些化合物的晶体学数据或对接研究,当有可用数据时,以提供对其作用机制的深入了解。

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