Recent Advances in the Discovery of Multitargeted Tyrosine Kinase Inhibitors as Anticancer Agents,ChemMedChem

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Recent Advances in the Discovery of Multitargeted Tyrosine Kinase Inhibitors as Anticancer Agents
ChemMedChem ( IF 3.6 ) Pub Date : 2020-11-12 , DOI: 10.1002/cmdc.202000658
Ting Guo ₁ , Shutao Ma ₁

Affiliation

The treatment of cancer has been one of the most significant challenges for the medical field. Further research on the signal transduction pathway of tumor cells is driving the rapid development of antitumor agents targeting tyrosine kinases. However, most of the currently approved tyrosine kinase inhibitors based on the “single target/single drug” design are becoming less and less effective in the treatment of complex, heterogeneous, and multigenic cancers; this also results in resistance to chemotherapy. In contrast, multitargeted tyrosine kinase inhibitors (MT‐TKIs) can effectively block multiple pathways of intracellular signal transduction. Therefore, they have therapeutic advantages over single‐targeted inhibitors and have become a hotspot in antitumor drug research in recent years. This minireview summarizes recent advances in the discovery of MT‐TKIs based on their chemical structures. In particular, we describe the kinase inhibitory and antitumor activity of promising compounds, as well as their structure – activity relationships (SARs).

中文翻译：

发现多靶点酪氨酸激酶抑制剂作为抗癌剂的最新进展

癌症的治疗一直是医学领域面临的最重大挑战之一。对肿瘤细胞信号转导通路的进一步研究正在推动以酪氨酸激酶为靶点的抗肿瘤药物的快速发展。然而，目前大多数批准的基于“单靶点/单药”设计的酪氨酸激酶抑制剂在治疗复杂、异质和多基因癌症方面的效果越来越差；这也会导致对化疗的抵抗。相比之下，多靶点酪氨酸激酶抑制剂（MT-TKI）可以有效阻断细胞内信号转导的多种途径。因此，它们比单靶向抑制剂具有治疗优势，成为近年来抗肿瘤药物研究的热点。这篇小综述总结了基于 MT-TKI 的化学结构发现它们的最新进展。特别是，我们描述了有希望的化合物的激酶抑制和抗肿瘤活性，以及它们的结构 - 活性关系 (SAR)。

更新日期：2020-11-12

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