Zhao Li-Ming, Xie Tian-Pei, He Yu-Qin, Xu De-Feng, Li Shao-Shun
School of Pharmacy, Shanghai Jiaotong University, 800 Dongchuan Road, Shanghai 200240, China.
Eur J Med Chem. 2009 Apr;44(4):1410-4. doi: 10.1016/j.ejmech.2008.09.039. Epub 2008 Oct 7.
In an attempt to develop potent and selective antitumor agents, a series of 6- and 2-(1-substituted-thio-4-methylpent-3-enyl)-5,8-dimethoxynaphthalene-1,4-diones were designed and synthesized. The cytotoxicities of these compounds were evaluated in vitro against BEL-7402, HT-29 and SPC-A1 cell lines. The pharmacological results showed that most of the prepared compounds displayed the excellent selective cytotoxicity toward HT-29 cells. From the structure-activity relationships we may conclude that the introduction of a thioether functional group at the 1'-position in the side chain of shikonin is associated with an increase in cytotoxicity.
为了开发高效且具选择性的抗肿瘤药物，设计并合成了一系列6-和2-(1-取代硫基-4-甲基戊-3-烯基)-5,8-二甲氧基萘-1,4-二酮。在体外评估了这些化合物对BEL-7402、HT-29和SPC-A1细胞系的细胞毒性。药理结果表明，大多数制备的化合物对HT-29细胞表现出优异的选择性细胞毒性。从构效关系我们可以得出结论，在紫草素侧链的1'-位引入硫醚官能团与细胞毒性的增加有关。
