新型β-咔啉衍生物的合成及其对五种肿瘤细胞系的活性。
Syntheses of novel β-carboline derivatives and the activities against five tumor-cell lines.
机构信息
Chinese Center for Chirality, The Key Laboratory of Medicinal Chemistry and Molecular Diagnostics, Department of Chemistry and Chemical Engineering, Hebei University, Baoding 071002, China; School of Food and Biological Engineering, Zhengzhou University of Light Industry, Zhengzhou 450002, China.
The State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, CAS, Kunming 650204, China.
出版信息
Bioorg Med Chem Lett. 2014 Jan 1;24(1):96-8. doi: 10.1016/j.bmcl.2013.11.076. Epub 2013 Dec 4.
A series of β-carbolines possessing the aryl group at C-1 position has been synthesized from tryptophan. The newly synthesized compounds were screened for their in vitro anticancer activity against various human cancer cell lines by MTT assay. Some of them exhibited anticancer activity with IC50 values lower than 10μM outdistanced the cisplatin level. Structure-activity relationship reveals that the alcohol substituents at C-3 position played an important role in inhibition activity.
一系列在 C-1 位置具有芳基取代基的β-咔啉类化合物已经从色氨酸中合成。新合成的化合物通过 MTT 法测定其对各种人癌细胞系的体外抗癌活性。其中一些化合物表现出抗癌活性，其 IC50 值低于 10μM，超过了顺铂的水平。构效关系表明，C-3 位的醇取代基在抑制活性中起着重要作用。
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