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Design and Synthesis of Biotinylated Bivalent Carboline Derivatives as Potent Antitumor Agents

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journal contribution
posted on 31.08.2020, 12:33 by Xueyuan Chen, Yi Zheng, Songlin Song, Ying Liu, Yi Wang, Yong Huang, Xiaoyi Zhang, Meng Zhang, Ming Zhao, Yuji Wang, Li Li
Compound 6, a novel β-carboline comprising two 1-methyl-9H-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 6 was delivered via biotin receptor-mediated endocytosis and exerted its therapeutic effects by intercalation binding with DNA. In vivo antitumor evaluations of 6 revealed that it is efficacious and exhibits low systemic toxicity.