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脱靶效应是癌症治疗面临的主要挑战，这促使药物化学家不断开发出更多高效、低毒的抗癌药物。磺胺类衍生物是一类很有前景的化合物，具有包括抗癌在内的多种生物活性，其中部分已上市用于癌症治疗，如 Belinostat、ABT-199 和 Amsacrine。在这篇综述中，我们根据芳香酶、碳酸酐酶（CA）、抗凋亡B细胞淋巴瘤2（Bcl-2）等抗癌靶点，总结了磺胺类衍生物作为潜在抗癌药物的最新进展。 ) 蛋白质、拓扑异构酶和磷脂酰肌醇 3-激酶 (PI3K)，并阐明了大多数磺胺衍生物的相应构效关系（SAR）。我们希望这篇综述可以为药物化学家在合理设计更有效和生物靶向特异性抗癌剂方面提供清晰的见解。