2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents.
2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents.
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DOI：
10.1016/j.ejmech.2020.112953
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发表时间：
2020-10
影响因子：
6.7
通讯作者：
Yichao Wan;Jiabing Long;Han Gao;Zilong Tang
中科院分区：
文献类型：
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作者：
Yichao Wan;Jiabing Long;Han Gao;Zilong Tang
癌症已成为人类社会仅次于心血管疾病的第二大健康杀手。尽管人们在癌症的治疗方面做出了许多努力，在癌症的诊断和治疗方面取得了许多成就，但由于多药耐药性和副作用的出现，目前的一线抗癌药物不足。因此，开发高效低毒的新型抗癌药物迫在眉睫。2-氨基噻唑是一类重要的骨架材料，广泛存在于天然和合成的化合物中，具有多种药理作用，包括潜在的抗癌活性。本文综述了近年来2-氨基噻唑作为一种特殊的骨架材料，在以微管蛋白、组蛋白乙酰化酶/组蛋白去乙酰化酶等生物靶点为基础的抗癌药物研究中的应用进展（HAT/HDAC）、磷脂酰肌醇3-激酶（PI 3 K）、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），并对大多数化合物的构效关系进行了研究。本文的综述有助于药物化学工作者发现更多具有良好活性和高治疗指数的2-氨基噻唑类抗癌药物。
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.