Design and Synthesis of Biotinylated Bivalent Carboline Derivatives as Potent Antitumor Agents
journal contributionposted 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.
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exhibitnovel β- carbolinetrisBiotinylated Bivalent Carboline Der...intercalation bindingMCF -71- methyl -9 H -β- carboline -3-car...S 180 tumor-bearing mouse modelbiotin receptor-mediated endocytosisSynthesivivo antitumor evaluationsDNAbiotin moietyHepG 2 cell linescytotoxicityPotent Antitumor AgentsCompound 6antitumor potencytoxicity