Motavallizadeh Somayeh, Fallah-Tafti Asal, Maleki Saeedeh, Shirazi Amir Nasrolahi, Pordeli Mahboobeh, Safavi Maliheh, Ardestani Sussan Kabudanian, Asd Shaaban, Tiwari Rakesh, Oh Donghoon, Shafiee Abbas, Foroumadi Alireza, Parang Keykavous, Akbarzadeh Tahmineh
Department of Medicinal Chemistry, Faculty of Pharmacy and Drug Design & Development Research Center, Tehran University of Medical Sciences, Tehran, Iran.
Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, Rhode Island, 02881, USA.
Tetrahedron Lett. 2014 Jan 8;55(2):373-375. doi: 10.1016/j.tetlet.2013.11.033.
Several novel -(9-oxo--xanthen-4-yl)benzenesulfonamides derivatives were prepared as potential antiproliferative agents. The 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-(9-oxo--xanthen-4-yl)benzenesulfonamide showed the highest antiproliferative activity against MDA-MB-231, T-47D, and SK-N-MC cells. Furthermore, pentafluoro derivatives and 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 development of new lead anticancer agents.
制备了几种新型的-(9-氧代-呫吨-4-基)苯磺酰胺衍生物作为潜在的抗增殖剂。使用MTT比色法研究了合成化合物对一组肿瘤细胞系的抗增殖活性，这些细胞系包括乳腺癌细胞系（MDA-MB-231、T-47D）和成神经细胞瘤细胞系（SK-N-MC）。依托泊苷，一种知名的抗癌药物，用作阳性标准药物。在合成化合物中，4-甲氧基-(9-氧代-呫吨-4-基)苯磺酰胺对MDA-MB-231、T-47D和SK-N-MC细胞表现出最高的抗增殖活性。此外，五氟衍生物对人白血病细胞系（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，呫吨苯磺酰胺杂化化合物可用于开发新型抗癌先导药物。
