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.

癌症已成为人类社会中仅次于心血管疾病的第二大健康杀手。尽管已经为癌症治疗做出了许多努力并且在癌症的诊断和治疗中已经获得了许多成就，但是由于出现了多药耐药性和副作用，当前的一线抗癌剂是不足的。因此，迫切需要开发具有高活性和低毒性的新型抗癌药。2-氨基噻唑是一类重要的支架，广泛分布在许多天然和合成化合物中，具有许多药理作用，包括潜在的抗癌活性。在这篇综述中，我们总结了2-氨基噻唑作为一种特权支架的最新进展，该支架用于发现基于生物靶标（例如微管蛋白）的抗癌药，组蛋白乙酰化酶/组蛋白脱乙酰基酶（HAT / HDAC），磷脂酰肌醇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），还研究了结构-活性关系（SAR）的大多数化合物。相信该综述对药物化学家发现更多具有优异活性和高治疗指数的2-氨基噻唑支架的抗癌药可能是有帮助的。