取代苯并咪唑基姜黄素类似物的合成及其抗癌活性。
Synthesis of substituted benzimidazolyl curcumin mimics and their anticancer activity.
机构信息
Department of Basic Science, Yonsei University Wonju College of Medicine, Wonju 220-701, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2012 Jan 15;22(2):933-6. doi: 10.1016/j.bmcl.2011.12.074. Epub 2011 Dec 20.
A novel curcumin mimic library (14a-14h and 15a-15h) possessing variously substituted benzimidazole groups was synthesized through the aldol reaction of (E)-4-(4-hydroxy-3-methoxyphenyl)but-3-en-2-one (7) or (E)-4-(3-hydroxy-4-methoxyphenyl)but-3-en-2-one (13) with diversely substituted benzimidazolyl-2-carbaldehyde (12a-12h). The MTT assay of the cancer cells MCF-7, SH-SY5Y, HEP-G2, and H460 showed that compound 14c with IC(50) of 1.0 and 1.9μM has a strong inhibitory effect on the growth of SH-SY5Y and Hep-G2 cells, respectively, and that compound 15h with IC(50) of 1.9μM has a strong inhibitory effect on the growth of MCF-7 cancer cells.
通过（E）-4-（4-羟基-3-甲氧基苯基）-3-丁烯-2-酮（7）或（E）-4-（3-羟基-4-甲氧基苯基）-3-丁烯-2-酮（13）与各种取代的苯并咪唑基-2-醛（12a-12h）的醛醇反应，合成了具有各种取代的苯并咪唑基团的新型姜黄素类似物库（14a-14h 和 15a-15h）。MTT 法测定 MCF-7、SH-SY5Y、HEP-G2 和 H460 癌细胞的结果表明，化合物 14c 的 IC50 分别为 1.0 和 1.9μM，对 SH-SY5Y 和 Hep-G2 细胞的生长具有很强的抑制作用，而化合物 15h 的 IC50 为 1.9μM，对 MCF-7 癌细胞的生长具有很强的抑制作用。
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