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Design, synthesis and cytotoxicity of novel hexacyclic saframycin–ecteinascidin analogs

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Abstract

Two series of novel hexacyclic skeletons and their thirty-four derivatives were prepared from L-tryptophan and L-DOPA. The cytotoxicities of these compounds were tested against four human cancer cell lines HCT-116, HepG2, BGC-823 and A2780. Compounds with the tetrahydro-β-carboline moiety in the left-half of the hexacyclic skeleton showed more potent cytotoxicity with IC50 values in the range of 10−7–10−9 M. Compound 20 with the 4-methoxybenzamide side chain showed potent cytotoxicity towards HepG2 with an IC50 value of 1.32 nM. Compounds 29 and 30 with 2-pyridine amide and (2E)-3-(3-thifluoromethyl-phenyl)acrylic amide side chains showed selective cytotoxicity towards A2780 with IC50 values of 1.73 nM and 7 nM, respectively.

Graphical abstract: Design, synthesis and cytotoxicity of novel hexacyclic saframycin–ecteinascidin analogs

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Publication details

The article was received on 11 Nov 2019, accepted on 22 Nov 2019 and first published on 22 Nov 2019


Article type: Paper
DOI: 10.1039/C9OB02426C
Org. Biomol. Chem., 2020, Advance Article

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    Design, synthesis and cytotoxicity of novel hexacyclic saframycin–ecteinascidin analogs

    X. Lu, X. Pan, B. Guan and Z. Liu, Org. Biomol. Chem., 2020, Advance Article , DOI: 10.1039/C9OB02426C

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