Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, School of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, P. R. China.
J Org Chem. 2020 Sep 18;85(18):11618-11625. doi: 10.1021/acs.joc.0c01067. Epub 2020 Aug 31.
Compound , a novel β-carboline comprising two 1-methyl-9-β-carboline-3-carboxylic acids and a biotin moiety conjugated together using tris(2-aminoethyl)amine, was synthesized and tested for its cytotoxicity toward MCF-7 and HepG2 cell lines and antitumor potency in an S180 tumor-bearing mouse model. Compound was delivered via biotin receptor-mediated endocytosis and exerted its therapeutic effects by intercalation binding with DNA. antitumor evaluations of revealed that it is efficacious and exhibits low systemic toxicity.
化合物是一种新型的β-咔啉，由两个 1-甲基-9-β-咔啉-3-羧酸和一个生物素部分通过三（2-氨基乙基）胺连接而成。该化合物已被合成并用于测试其对 MCF-7 和 HepG2 细胞系的细胞毒性以及在 S180 荷瘤小鼠模型中的抗肿瘤活性。化合物通过生物素受体介导的内吞作用传递，并通过与 DNA 的插入结合发挥其治疗作用。化合物的抗肿瘤评估表明，它具有疗效且全身毒性低。
