癌症是世界范围内死亡和发病的主要原因之一。大量的研究工作已经进行，以开发具有更好抗癌功效的新化学物质。2-氨基苯并噻唑是一类重要的杂环化合物，它含有一个硫和两个氮原子，与广泛的医学和药理活性相关，包括抗肿瘤、抗菌、抗疟疾、抗炎和抗病毒活性。近年来，一批具有强大的、低毒的2-氨基苯并噻唑化合物被发现作为新的抗癌剂。在这里，我们基于它们对肿瘤相关蛋白的活性（包括酪氨酸激酶（CSF1R、EGFR、VEGFR-2、FAK和MET）、丝氨酸/苏氨酸激酶（Aurora、CDK、CK、RAF和DYRK2）、PI3K激酶、BCL-XL、HSP90、突变p53蛋白、DNA拓扑异构酶、HDAC、NSD1、LSD1、FTO、mPGES-1、SCD、hCA IX/XII和CXCR）提供了这类化合物的综合评价。此外，本文还描述了2-氨基苯并噻唑衍生螯合剂和金属配合物的抗癌潜力。此外，本文还广泛评述了2-氨基苯并噻唑作为新型抗癌剂的设计策略、作用机理、结构活性关系（SAR）和更高级别的临床前开发阶段。最后，突出了2-氨基苯并噻唑相对其他杂环系统具有优势的例子。版权所有©2023 Elsevier Inc.。保留所有权利。

Cancer is one of the major causes of mortality and morbidity worldwide. Substantial research efforts have been made to develop new chemical entities with improved anticancer efficacy. 2-Aminobenzothiazole is an important class of heterocycles containing one sulfur and two nitrogen atoms, which is associated with a broad spectrum of medical and pharmacological activities, including antitumor, antibacterial, antimalarial, anti-inflammatory, and antiviral activities. In recent years, an extraordinary collection of potent and low-toxicity 2-aminobenzothiazole compounds have been discovered as new anticancer agents. Herein, we provide a comprehensive review of this class of compounds based on their activities against tumor-related proteins, including tyrosine kinases (CSF1R, EGFR, VEGFR-2, FAK, and MET), serine/threonine kinases (Aurora, CDK, CK, RAF, and DYRK2), PI3K kinase, BCL-XL, HSP90, mutant p53 protein, DNA topoisomerase, HDAC, NSD1, LSD1, FTO, mPGES-1, SCD, hCA IX/XII, and CXCR. In addition, the anticancer potentials of 2-aminobenzothiazole-derived chelators and metal complexes are also described here. Moreover, the design strategies, mechanism of actions, structure-activity relationships (SAR) and more advanced stages of pre-clinical development of 2-aminobenzothiazoles as new anticancer agents are extensively reviewed in this article. Finally, the examples that 2-aminobenzothiazoles showcase an advantage over other heterocyclic systems are also highlighted.Copyright © 2023 Elsevier Inc. All rights reserved.