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2-氨基噻唑衍生物在抗癌药物研发中的进展及治疗潜力

Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery.

作者信息

Alizadeh Seyedeh Roya, Hashemi Seyedeh Mahdieh

机构信息

Student Research Committee, Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.

Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.

出版信息

Med Chem Res. 2021;30(4):771-806. doi: 10.1007/s00044-020-02686-2. Epub 2021 Jan 15.

Abstract

Currently, the development of anticancer drug resistance is significantly restricted the clinical efficacy of the most commonly prescribed anticancer drug. Malignant disease is widely prevalent and considered to be the major challenges of this century, which concerns the medical community all over the world. Consequently, investigating small molecule antitumor agents, which could decrease drug resistance and reduce unpleasant side effect is more desirable. 2-aminothiazole scaffold has emerged as a promising scaffold in medicinal chemistry and drug discovery research. This nucleus is a fundamental part of some clinically applied anticancer drugs such as dasatinib and alpelisib. Literature survey documented that different 2-aminothiazole analogs exhibited their potent and selective nanomolar inhibitory activity against a wide range of human cancerous cell lines such as breast, leukemia, lung, colon, CNS, melanoma, ovarian, renal, and prostate. In this paper, we have reviewed the progresses and structural modification of 2-aminothiazole to pursuit potent anticancers and also highlighted in vitro activities and in silico studies. The information will useful for future innovation. Representatives of 2-aminothiazole-containing compounds classification.

摘要

目前,抗癌药物耐药性的发展严重限制了最常用抗癌药物的临床疗效。恶性疾病广泛流行,被认为是本世纪的主要挑战,这引起了全世界医学界的关注。因此,研究能够降低耐药性并减少不良副作用的小分子抗肿瘤药物更具吸引力。2-氨基噻唑骨架已成为药物化学和药物发现研究中一种有前景的骨架。这个核心是一些临床应用的抗癌药物如达沙替尼和阿哌利西的基本组成部分。文献调查表明,不同的2-氨基噻唑类似物对多种人类癌细胞系,如乳腺癌、白血病、肺癌、结肠癌、中枢神经系统癌、黑色素瘤、卵巢癌、肾癌和前列腺癌,表现出强效且选择性的纳摩尔抑制活性。在本文中,我们综述了2-氨基噻唑为寻求强效抗癌药物所取得的进展和结构修饰,还强调了体外活性和计算机模拟研究。这些信息将对未来的创新有用。含2-氨基噻唑化合物分类的代表。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1050/7809097/59200a06dde2/44_2020_2686_Figa_HTML.jpg

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