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引用次数: 0
摘要
表皮生长因子受体(FGFR)已被证明在生物过程中起着至关重要的作用,但它们的过度表达已被认为是导致不同类型癌症发生和发展的操作成分。在所有围绕癌症的研究中,表皮生长因子受体(FGFR)抑制剂在过去几年中迅速崛起。因此,表皮生长因子受体抑制剂是逆转耐药性、肿瘤生长和血管生成的主要基本工具之一。目前,许多 FGFR 抑制剂正处于开发阶段或已经开发出来。由于需求大、热点多,人们通过不同的药理机制来获得结构多样的表皮生长因子受体(FGFR)抑制剂。在此,我们选择了几个具有代表性的例子,如萘基、嘧啶、哒嗪、吲哚和喹啉衍生物,以说明 FGFR 抑制剂在药物化学中的多样性和进展。本综述重点介绍了过去五年来对表皮生长因子受体(FGFR)抑制剂的 SAR 研究,这将是一个巨大的未来空间,影响着药物化学家在这一领域取得更多成就。
A Promising Paradigm Shift in Cancer Treatment with FGFR Inhibitors.
FGFR have been demonstrated to perform a crucial role in biological processes but their overexpression has been perceived as the operator component in the occurrence and progression of different types of carcinoma. Out of all the interest around cancer, FGFR inhibitors have assembled pace over the past few years. Therefore, FGFR inhibitors are one of the main fundamental tools to reverse drug resistance, tumor growth, and angiogenesis. Currently, many FGFR inhibitors are under the development stage or have been developed. Due to great demand and hotspots, different pharmacophores were approached to access structurally diverse FGFR inhibitors. Here, we have selected to present several representative examples such as Naphthyl, Pyrimidine, Pyridazine, Indole, and Quinoline derivatives that illustrate the diversity and advances of FGFR inhibitors in medicinal chemistry. This review focuses on the SAR study of FGFR inhibitors last five years which will be a great future scope that influences the medicinal chemist to work towards more achievements in this area.
期刊介绍:
Formerly: Current Medicinal Chemistry - Anti-Cancer Agents.
Anti-Cancer Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of anti-cancer agents.
Each issue contains a series of timely in-depth reviews and guest edited issues written by leaders in the field covering a range of current topics in cancer medicinal chemistry. The journal only considers high quality research papers for publication.
Anti-Cancer Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in cancer drug discovery.