کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1395167 | 1501202 | 2009 | 5 صفحه PDF | دانلود رایگان |

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.
The synthesis, biological evaluation and structure–activity relationships of 6- and 2-(1-substituted-thiol-4-methylpent-3-enyl)-5,8-dimethoxynaphthalene-1,4-diones as antitumor agents are reported.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 44, Issue 4, April 2009, Pages 1410–1414