细胞增殖异常是癌症的最初症状,最终会转移到其他器官。在癌症转移之前,它的传播是由包括血管内皮生长因子受体(VEGFR)在内的促血管生成因子触发的,表皮生长因子受体(EGFR),血小板衍生生长因子受体(PDGFR),成纤维细胞生长因子受体(FGFR)和血小板因子(PF4),所有这些都是受体酪氨酸激酶(RTK)家族的一部分。受体酪氨酸激酶(RTK)是细胞表面蛋白和信号酶,将ATP-磷酸转移到酪氨酸残基底物。重要的生物过程,如增殖,分化,运动性,和细胞周期调控都是这些蛋白质所拥有的。异常的RTK表达通常与细胞生长异常有关,这与肿瘤的获得有关,血管生成,和癌症进展。除了现有的药物,正在研究许多其他杂环对多种癌症的潜在作用。在与癌症的斗争中,特别是,这些杂环已被用于其动态核心支架及其固有的适应性。在这篇评论文章中,我们已经汇编了过去五年的研究工作,包括针对RTK的含氮杂环。在这里,含有多种杂环(嘧啶,吲哚,吡啶,吡唑,苯并咪唑,和吡咯)支架进行了讨论,并且它们可能在将来被证明对设计针对RTK的新线索有用。本文的重点是全面综述含氮化合物作为RTK抑制剂的生物活性和结构活性关系的最新研究。我们认为这可能是对该领域的重要贡献,因为它可以帮助指导未来的研究工作,并促进开发更有效的癌症疗法。
Erratic cell proliferation is the initial symptom of cancer, which can eventually metastasize to other organs. Before cancer becomes metastatic, its spread is triggered by pro-angiogenic factors including vascular endothelial growth factor receptor (VEGFR), epidermal growth factor receptor (EGFR), Platelet-derived growth factor receptor (PDGFR), fibroblast growth factor receptor (FGFR) and Platelet Factor (PF4), all of which are part of receptor tyrosine kinase (RTK) family. Receptor tyrosine kinases (RTKs) are cell-surface proteins and aresignaling enzymes that transfer ATP-phosphate to tyrosine residue substrates. Important biological processes like proliferation, differentiation, motility, and cell-cycle regulation are all possessedby these proteins. Unusual RTK expression is typically associated with cell growth abnormalities, which is linked to tumor acquisition, angiogenesis, and cancer progression. In addition to the already available medications, numerous other heterocyclic are being studied for their potential action against a variety of cancers. In the fight against cancer, in particular, these heterocycles have been used for their dynamic core scaffold and their inherent adaptability. In this review article, we have compiled last five years research work including nitrogen containing heterocycles that have targeted RTK. Herein, the SAR and activity of various compounds containing diverse heterocyclic (pyrimidine, indole, pyridine, pyrazole, benzimidazole, and pyrrole) scaffolds are discussed, and they may prove useful in the future for designing new leads against RTKs. Our focus in this manuscript is to comprehensively review the latest research on the biological activity and structural activity relationship of nitrogen compounds as RTK inhibitors. We believe that this may be an important contribution to the field, as it can help guide future research efforts and facilitate the development of more effective cancer therapies.