Several novel N-(9-oxo-9H-xanthen-4-yl)benzenesulfonamide derivatives were prepared as potential antiproliferative agents. The in vitro antiproliferative activity of the synthesized compounds was investigated against a panel of tumor cell lines including breast cancer cell lines (MDA-MB-231, T-47D) and neuroblastoma cell line (SK-N-MC) using MTT colorimetric assay. Etoposide, a well-known anticancer drug, was used as a positive standard drug. Among synthesized compounds, 4-methoxy-N-(9-oxo-9H-xanthen-4-yl)benzenesulfonamide (5i) showed the highest antiproliferative activity against MDA-MB-231, T-47D, and SK-N-MC cells. Furthermore, pentafluoro derivatives 5a and 6a exhibited higher antiproliferative activity than doxorubicin against human leukemia cell line (CCRF-CEM) and breast adenocarcinoma (MDA-MB-468) cells. Structure–activity relationship studies revealed that xanthone benzenesulfonamide hybrid compounds can be used for the development of new lead anticancer agents.

制备了几种新型N -(9- oxo- 9H -xanthen-4-yl) 苯磺酰胺衍生物作为潜在的抗增殖剂。使用 MTT 比色法研究合成化合物对一组肿瘤细胞系的体外抗增殖活性，包括乳腺癌细胞系（MDA-MB-231、T-47D）和神经母细胞瘤细胞系（SK-N-MC）。依托泊苷是一种著名的抗癌药物，被用作阳性标准药物。在合成的化合物中，4-甲氧基-N-（9-氧代-9H -xanthen-4-yl）苯磺酰胺（5i）对MDA-MB-231、T-47D和SK-N-MC细胞显示出最高的抗增殖活性. 此外，五氟衍生物5a和6a对人白血病细胞系（CCRF-CEM）和乳腺腺癌（MDA-MB-468）细胞表现出比阿霉素更高的抗增殖活性。构效关系研究表明，氧杂蒽酮苯磺酰胺杂化化合物可用于开发新的先导抗癌药物。