Key Laboratory of Theoretical Organic Chemistry and Functional Molecule, Ministry of Education, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China; Hunan Provincial Key Laboratory of Controllable Preparation and Functional Application of Fine Polymers, Hunan Provincial Key Lab of Advanced Materials for New Energy Storage and Conversion, School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China.
Key Laboratory of Theoretical Organic Chemistry and Functional Molecule, Ministry of Education, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China; Hunan Provincial Key Laboratory of Controllable Preparation and Functional Application of Fine Polymers, Hunan Provincial Key Lab of Advanced Materials for New Energy Storage and Conversion, School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan, Hunan, 411201, PR China.
Eur J Med Chem. 2021 Dec 15;226:113837. doi: 10.1016/j.ejmech.2021.113837. Epub 2021 Sep 8.
Currently, the arise of drug resistance and undesirable off-target effects of anti-cancer agents are major challenges for cancer treatment, which energizes medicinal chemists to develop more anti-cancer agents with high efficiency and low toxicity continuously. Sulfonamide derivatives are a class of promising compounds with diverse biological activities including anti-cancer, and parts of them have been marketed for cancer therapy, such as Belinostat, ABT-199 and Amsacrine. In this review, we summed up the recent advances of sulfonamide derivatives as potential anti-cancer agents based on the anti-cancer targets, such as aromatase, carbonic anhydrase (CA), anti-apoptotic B-cell lymphoma-2 (Bcl-2) proteins, topoisomerase and phosphatidylinositol 3-kinase (PI3K), and elucidated the corresponding structure-activity relationships (SARs) of most sulfonamide derivatives. We hope this review could provide a clear insight for medicinal chemists in the rational design of more potent and bio-target specific anti-cancer agents.
目前，抗癌药物的耐药性和不良的非靶标效应的出现是癌症治疗的主要挑战，这促使药物化学家不断开发高效低毒的新型抗癌药物。磺酰胺衍生物是一类具有多种生物活性的化合物，包括抗癌活性，其中部分已上市用于癌症治疗，如贝林司他、 ABT-199 和安吖啶。在本文中，我们根据芳香酶、碳酸酐酶（CA）、抗凋亡 B 细胞淋巴瘤-2（Bcl-2）蛋白、拓扑异构酶和磷脂酰肌醇 3-激酶（PI3K）等抗癌靶点，总结了磺酰胺衍生物作为潜在抗癌药物的最新进展，并阐明了大多数磺酰胺衍生物的相应构效关系（SAR）。我们希望这篇综述能为药物化学家合理设计更有效、更具生物靶向性的抗癌药物提供清晰的思路。
