Department of Chemistry, College of Science, Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia.
Chemistry of Natural Compounds Department, National Research Centre, Dokki, Egypt.
Bioorg Chem. 2020 Oct;103:104163. doi: 10.1016/j.bioorg.2020.104163. Epub 2020 Aug 26.
Heading the list of the critical health-related issues worldwide, cancer continues to be a one of the most serious life-threatening diseases. The rate of cancer-related mortality is at alarming level globally because of poor ability of prevention, diagnosis and efficient treatment of cancers. Pertaining to its wide prevalence in many naturally occurring compounds, coumarin as a privileged scaffold is endowed with outstanding anticancer profile. Different classes of coumarin-based anticancer agents that act through diverse mechanisms of action have been comprehensively investigated by many researchers, such as alkylating agents, topoisomerase inhibitors, hormone antagonists, angiogenesis inhibitors, antimitotic agents, apoptosis inducers, human carbonic anhydrase inhibitors, telomerase inhibitors and other mechanisms. Accordingly, medicinal chemists and drug design scientists embarked on exploring diverse coumarin-based derivatives comprehending their potential to develop new efficient anticancer agents. The present review provides an overview of different anticancer classes based on the coumarin scaffold that have been reported since 2015 with particular emphasis on their cellular and enzymatic mechanism of actions.
在全球与健康相关的重大问题中,癌症仍然是最严重的威胁生命的疾病之一。由于癌症的预防、诊断和有效治疗能力差,全球癌症相关死亡率处于令人震惊的水平。香豆素作为一种特权支架,由于其在许多天然存在的化合物中的广泛存在,具有出色的抗癌特性。许多研究人员对不同类别的基于香豆素的抗癌药物进行了全面研究,这些药物通过不同的作用机制发挥作用,例如烷化剂、拓扑异构酶抑制剂、激素拮抗剂、血管生成抑制剂、抗有丝分裂剂、凋亡诱导剂、人碳酸酐酶抑制剂、端粒酶抑制剂和其他机制。因此,药物化学家们和药物设计科学家们开始探索各种基于香豆素的衍生物,以了解其开发新型有效抗癌药物的潜力。本综述提供了自 2015 年以来基于香豆素支架的不同抗癌类别的概述,特别强调了它们的细胞和酶作用机制。