新型姜黄素单羰基类似物的合成、抗疟活性和细胞毒性潜力。

Synthesis, antimalarial activity and cytotoxic potential of new monocarbonyl analogues of curcumin.

机构信息

Department of Chemistry, University of Delhi, Delhi 110007, India.

出版信息

Bioorg Med Chem Lett. 2013 Jan 1;23(1):112-6. doi: 10.1016/j.bmcl.2012.11.004. Epub 2012 Nov 10.

DOI:10.1016/j.bmcl.2012.11.004

Abstract

A series of novel monocarbonyl analogues of curcumin have been designed, synthesized and tested for their activity against Molt4, HeLa, PC3, DU145 and KB cancer cell lines. Six of the analogues showed potent cytotoxicity towards these cell lines with IC(50) values below 1 μM, which is better than doxorubicin, a US FDA approved drug. Several analogues were also found to be active against both CQ-resistant (W2 clone) and CQ-sensitive (D6) strains of Plasmodium falciparum in an in-vitro antimalarial screening. This level of activity warrants further investigation of the compounds for development as anticancer and antimalarial agents.

摘要

已经设计、合成并测试了一系列新型姜黄素单羰基类似物，以评估其对 Molt4、HeLa、PC3、DU145 和 KB 癌细胞系的活性。其中 6 种类似物对这些细胞系表现出很强的细胞毒性，IC50 值低于 1 μM，优于美国食品和药物管理局批准的药物多柔比星。在体外抗疟筛选中，几种类似物对耐氯喹（W2 克隆）和敏感（D6）疟原虫菌株也具有活性。这种活性水平表明有必要进一步研究这些化合物，以开发它们作为抗癌和抗疟药物。