Petrosian Artem, Pinheiro Pedro F, Ribeiro Ana P C, Martins Luísa M D R S, Justino Gonçalo C
Centro de Química Estrutural-Institute of Molecular Sciences, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais, 1, 1049-001 Lisboa, Portugal.
Escola Superior de Tecnologia do Barreiro, Instituto Politécnico de Setúbal, Rua Américo da Silva Marinho, 2839-001 Lavradio, Portugal.
Molecules. 2024 Nov 30;29(23):5672. doi: 10.3390/molecules29235672.
Cancer remains a formidable challenge, requiring the constant pursuit of novel therapeutic agents and strategies. Scorpionates, known for their unique coordination properties, have recently gained attention for their anticancer potential. Traditionally applied in catalysis, these compounds have demonstrated notable cytotoxicity across various cancer cell lines, often surpassing the efficacy of conventional chemotherapeutics. This review addresses recent findings on scorpionate complexes, emphasizing the impact of metal choice and ligand design on biological activity. Copper and ruthenium scorpionates show promise, leveraging redox activity and mitochondrial disruption mechanisms to selectively induce cancer cell death. Ligand modifications, including sulfur-containing heterocycles and unsubstituted pyrazoles, have proven effective in enhancing cytotoxicity and selectivity. Furthermore, dipodal ligands show unique potential, with selective binding sites that improve stability and facilitate specific cellular interactions, such as targeting metastatic pathways. These findings highlight the largely unexplored potential of scorpionate complexes, positioning them as candidates for next-generation anticancer therapies. Continued research into structure-activity relationships and precise mechanisms of action could pave the way for developing highly potent and selective anticancer agents based on scorpionate chemistry.
癌症仍然是一项艰巨的挑战，需要不断探索新型治疗药物和策略。蝎形化合物以其独特的配位特性而闻名，最近因其抗癌潜力而受到关注。这些化合物传统上应用于催化领域，已在多种癌细胞系中显示出显著的细胞毒性，其疗效往往超过传统化疗药物。本综述阐述了蝎形配合物的最新研究成果，重点强调了金属选择和配体设计对生物活性的影响。含铜和钌的蝎形化合物显示出应用前景，它们利用氧化还原活性和线粒体破坏机制选择性地诱导癌细胞死亡。包括含硫杂环和未取代吡唑在内的配体修饰已被证明能有效增强细胞毒性和选择性。此外，双齿配体显示出独特的潜力，其选择性结合位点可提高稳定性并促进特定的细胞相互作用，如靶向转移途径。这些发现凸显了蝎形配合物在很大程度上尚未被探索的潜力，使其成为下一代抗癌疗法的候选药物。对构效关系和精确作用机制的持续研究可能为基于蝎形化学开发高效、选择性抗癌药物铺平道路。
