School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan 430074, China.
Hubei Key Laboratory of Radiation Chemistry and Functional Materials, Non-power Nuclear Technology Collaborative Innovation Centre, School of Nuclear Technology and Chemistry & Biology, Hubei University of Science and Technology, Xianning 437100, China.
Curr Top Med Chem. 2021;21(19):1725-1736. doi: 10.2174/1568026620999201113110041.
Cancer is the main cause of death, and the emergence of resistance by cancer cells towards existing anticancer agents is one of the major problems for effective chemotherapy, creating a great demand for the development of novel anticancer drugs. Coumarins, abundantly found in nature, constitute an important class of pharmacological agents possessing physiological activities. The mechanism investigations elucidated that coumarins could lead to self-programmed cancer cell death (apoptosis) via different mechanisms; thereby coumarin-based derivatives possess potential activity against various forms of cancers, including drug-resistant, even multidrug-resistant cancers. This review article describes the recent progress in the discovery, structural modification, structure-activity relationship, and mechanism of action studies of coumarin-based derivatives with potential activity against drug-resistant cancers, covering articles published between 2010 and 2020.
癌症是主要的死亡原因，癌细胞对现有抗癌药物的耐药性的出现是有效化疗的主要问题之一，这就需要开发新型抗癌药物。香豆素在自然界中大量存在，是具有生理活性的一类重要的药物。机制研究表明，香豆素可以通过不同的机制导致细胞的自我编程性死亡（细胞凋亡）；因此，基于香豆素的衍生物具有针对各种形式的癌症的潜在活性，包括耐药性，甚至多药耐药性癌症。本文综述了 2010 年至 2020 年期间发表的具有抗耐药性癌症活性的香豆素类衍生物的发现、结构修饰、构效关系和作用机制研究的最新进展。
