Asmaa E. Kassab, Rania M. Gomaa and Ehab M. Gedawy
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A substantial body of research documented the cytotoxic potential of experimental fluoroquinolones (FQs) on tumor cell lines and their remarkable efficacy against eukaryotic Topo II in addition to optimized physical and metabolic characteristics. The FQ scaffold has a unique ability to potentially resolve every major issue associated with traditional Topo II inhibitors while maintaining a highly desirable profile in crucial drug-likeness parameters; therefore, there is a significant chance that FQs will be repositioned as anticancer candidates. This review offers a summary of the most recent research on the anticancer potential of FQs that was published in 2023. 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引用次数: 0
摘要
目前,药品开发商正集中精力研究替代战略,如 "药品重新定位",以解决与生产率、监管障碍和药品成本稳步上升有关的问题。重新定位是停止寻找新药的最佳策略,因为为已获批准或不成功的药物研究新的适应症所需的时间和资金都较少。尽管目前市场上已有几种强效的 Topo II 抑制剂作为治疗多种癌症的重要药物,但未来可能还需要更多的药物。目前的抑制剂存在一些缺点,包括获得性抗药性和不利的副作用,如心脏毒性和随后的恶性肿瘤。大量研究记录了实验性氟喹诺酮类药物(FQs)对肿瘤细胞系的细胞毒性潜力及其对真核拓扑 II 的显著疗效,以及优化的物理和代谢特性。FQ 支架具有独特的能力,有可能解决与传统 Topo II 抑制剂相关的所有主要问题,同时在关键的药物相似性参数方面保持非常理想的特征;因此,FQs 有很大机会被重新定位为抗癌候选药物。本综述概述了 2023 年发表的有关 FQs 抗癌潜力的最新研究。除了讨论结构活性关系研究及其抗增殖活性的机制外,本综述还旨在提供最新信息,促进开发更有效的 FQs,使其成为可行的癌症治疗候选药物。
Drug repurposing of fluoroquinolones as anticancer agents in 2023
Drug developers are currently focusing on investigating alternative strategies, such as “drug repositioning”, to address issues associated with productivity, regulatory obstacles, and the steadily rising cost of pharmaceuticals. Repositioning is the best strategy to stop searching for new drugs because it takes less time and money to investigate new indications for already approved or unsuccessful drugs. Although there are several potent Topo II inhibitors available on the market as important drugs used in the therapy of many types of cancer, more may be required in the future. The current inhibitors have drawbacks including acquired resistance and unfavorable side effects such as cardiotoxicity and subsequent malignancy. A substantial body of research documented the cytotoxic potential of experimental fluoroquinolones (FQs) on tumor cell lines and their remarkable efficacy against eukaryotic Topo II in addition to optimized physical and metabolic characteristics. The FQ scaffold has a unique ability to potentially resolve every major issue associated with traditional Topo II inhibitors while maintaining a highly desirable profile in crucial drug-likeness parameters; therefore, there is a significant chance that FQs will be repositioned as anticancer candidates. This review offers a summary of the most recent research on the anticancer potential of FQs that was published in 2023. Along with discussing structural activity relationship studies and the mechanism underlying their antiproliferative activity, this review aims to provide up-to-date information that will spur the development of more potent FQs as viable cancer treatment candidates.
期刊介绍:
An international, peer-reviewed journal covering all of the chemical sciences, including multidisciplinary and emerging areas. RSC Advances is a gold open access journal allowing researchers free access to research articles, and offering an affordable open access publishing option for authors around the world.