Cytotoxicities of the quinolizidine alkaloid (–)-cytisine and 19 of its derivatives with substituents in the 3-, 9-, and 11-positions were assessed against A431 (epidermal carcinoma), A375 (melanoma), and HCT 116 (colorectal carcinoma) tumor cell lines using the MTT assay (etoposide reference drug). Practically all synthesized compounds at a concentration of 30 μM possessed slight ability to inhibit metabolic activity of these cell lines except benzylcytisine 4, methylcytisines 18 and 19, which contained a phenylurea fragment in the 9- or 11-position of the 2-pyridone core, and 11-chloro adamantylthiocarboxamide 16. Thiocarboxamide 16 reduced A431 cell survival up to 56.06% under the experimental conditions; derivatives 4, 18, and 19, of HCT 116 cell line by 57.52, 58.84, and 56.34%, respectively.
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The work was sponsored by a State Task for UfIC, UFRC, RAS, Topic No. AAAA-A20-120012090026-9.
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Translated from Khimiya Prirodnykh Soedinenii, No. 5, September–October, 2020, pp. 763–766.
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Petrova, P.R., Koval′skaya, A.V., Tsypysheva, I.P. et al. Synthesis of Several Cytisine Derivatives and their Cytotoxicities against A431, A375, and HCT 116 Tumor Cell Lines. Chem Nat Compd 56, 892–895 (2020). https://doi.org/10.1007/s10600-020-03177-x
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DOI: https://doi.org/10.1007/s10600-020-03177-x