Mehra Anuradha, Sangwan Rekha
Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Lovely Professional University, Jalandhar-Delhi G.T. Road (NH-1), Phagwara (Punjab), 144411, India.
Anticancer Agents Med Chem. 2025;25(1):2-23. doi: 10.2174/0118715206318833240819031953.
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.
成纤维细胞生长因子受体（FGFR）已被证明在生物过程中发挥关键作用，但其过表达被视为不同类型癌症发生和发展的驱动因素。在围绕癌症的所有研究热点中，FGFR抑制剂在过去几年里发展迅速。因此，FGFR抑制剂是逆转耐药性、肿瘤生长和血管生成的主要基础工具之一。目前，许多FGFR抑制剂正处于研发阶段或已研发成功。由于巨大的需求和研究热点，人们采用了不同的药效基团来获得结构多样的FGFR抑制剂。在此，我们选择展示几个代表性的例子，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。本综述重点关注过去五年FGFR抑制剂的构效关系研究，这将是一个广阔的未来研究领域，有望激励药物化学家在该领域取得更多成果。
