Key Laboratory of Theoretical Organic Chemistry and Functional Molecule, Ministry of Education, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China; Hunan Provincial Key Laboratory of Controllable Preparation and Functional Application of Fine Polymers, Hunan Provincial Key Lab of Advanced Materials for New Energy Storage and Conversion, School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China.
Key Laboratory of Theoretical Organic Chemistry and Functional Molecule, Ministry of Education, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China; Hunan Provincial Key Laboratory of Controllable Preparation and Functional Application of Fine Polymers, Hunan Provincial Key Lab of Advanced Materials for New Energy Storage and Conversion, School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China.
Eur J Med Chem. 2021 Jan 15;210:112953. doi: 10.1016/j.ejmech.2020.112953. Epub 2020 Oct 29.
Cancer has been the second heath killer being next only to cardiovascular diseases in human society. Although many efforts have been taken for cancer therapy and many achievements have been yielded in the diagnosis and treatment of cancer, the current first-line anti-cancer agents are insufficient owing to the emergence of multi-drug resistance and side effects. Therefore, it is urgent to develop new anti-cancer agents with high activity and low toxicity. 2-Aminothiazole is a class of important scaffold which widely distributes in many natural and synthetic compounds with many pharmacological effects including the potential anti-cancer activity. In this review, we summarized the recent progress of 2-aminothiazole as a privileged scaffold for the discovery of anti-cancer agents based on biological targets, such as tubulin protein, histone acetylase/histone deacetylase (HAT/HDAC), phosphatidylinositol 3-kinases (PI3Ks), Src/Abl kinase, BRAF kinase, epidermal growth factor receptor (EGFR) kinase and sphingosine kinase (SphK), and also investigated the structure-activity relationships (SARs) of most compounds. It is believed that this review could be helpful for medicinal chemists in the discovery of more anti-cancer agents bearing 2-aminothiazole scaffold with excellent activity and high therapeutic index.
癌症是人类社会仅次于心血管疾病的第二大健康杀手。尽管在癌症治疗方面已经做出了许多努力，并且在癌症的诊断和治疗方面取得了许多成果，但由于多药耐药性和副作用的出现，目前的一线抗癌药物仍然不足。因此，迫切需要开发具有高活性和低毒性的新型抗癌药物。2-氨基噻唑是一类重要的结构骨架，广泛分布于许多天然和合成化合物中，具有多种药理作用，包括潜在的抗癌活性。在这篇综述中，我们根据生物靶点，如微管蛋白、组蛋白乙酰转移酶/组蛋白去乙酰化酶（HAT/HDAC）、磷酸肌醇 3-激酶（PI3Ks）、Src/Abl 激酶、BRAF 激酶、表皮生长因子受体（EGFR）激酶和鞘氨醇激酶（SphK），总结了 2-氨基噻唑作为发现抗癌药物的优势骨架的最新进展，同时还研究了大多数化合物的结构-活性关系（SARs）。相信这篇综述可以为药物化学家发现更多具有 2-氨基噻唑骨架的、活性优异、治疗指数高的抗癌药物提供帮助。
