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综述类呋喃并[2,3-d]嘧啶酮衍生物的抗癌活性及其构效关系(SAR)研究进展

Review of anticancer potentials and structure-activity relationships (SAR) of rhodanine derivatives.

机构信息

School of Pharmacy, International Medical University (IMU), Kuala Lumpur 57000, Malaysia.

Department of Pharmaceutical Chemistry, School of Pharmacy, International Medical University (IMU), Kuala Lumpur 57000, Malaysia; Centre for Bioactive Molecules and Drug Delivery, Institute for Research, Development and Innovation (IRDI), International Medical University (IMU), Kuala Lumpur 57000, Malaysia.

出版信息

Biomed Pharmacother. 2022 Jan;145:112406. doi: 10.1016/j.biopha.2021.112406. Epub 2021 Nov 13.

Abstract

Rhodanine has been recognized as a privileged scaffold in medicinal chemistry due to its well-known ability to demonstrate a broad range of biological activities. The possibility of structural diversification has contributed to the significance of rhodanine structure in effective drug discovery and design. Many studies have confirmed the potential of rhodanine-derived compounds in the treatment of different types of cancer through the apoptosis induction mechanism. Furthermore, most of the rhodanine derivatives exhibited remarkable anticancer activity in the micromolar range while causing negligible cytotoxicity to normal cells. This review critically describes the anticancer activity profile of reported rhodanine compounds and the structure-activity relationships (SAR) to highlight the value of rhodanine as the core structure for future cancer drug development as well as to assist the researchers in rational drug design.

摘要

由于其具有广泛的生物活性,硫代吗啉已被公认为药物化学中的一种重要结构。其结构多样化的可能性使其在有效的药物发现和设计中具有重要意义。许多研究证实,通过诱导细胞凋亡的机制,硫代吗啉类化合物在治疗多种类型的癌症方面具有潜在作用。此外,大多数硫代吗啉衍生物在微摩尔浓度范围内表现出显著的抗癌活性,而对正常细胞的细胞毒性可忽略不计。本综述批判性地描述了已报道的硫代吗啉类化合物的抗癌活性特征和构效关系(SAR),以突出硫代吗啉作为未来癌症药物开发核心结构的价值,并帮助研究人员进行合理的药物设计。

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