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The Synthesis and Selective Cytotoxicity of New Mannich Bases, Derivatives of 19- and 28-Alkynyltriterpenoids

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Abstract

New propargylamines were synthesized in 72–75% yields by the interaction of 19-alkynylbetulin and 28-O-propargyl glycinamide of oleanolic acid with N-methylpiperazine under the Mannich reaction conditions. 19-[1-Methyl-4-prop-2-yn-1-yl-piperazine]-20,29,30-trinorbetulin was shown to manifest anticancer activity against one line of leukemia cells and two lines of colon cancer cells, whereas the growth of leukemia cells SR in the presence of 4-(4-methylpiperazin-1-yl)but-2-yn-1-yl-N-(3-hydroxy-28-oxoolean-12-en-28-yl)glycinate was 8%.

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Correspondence to E. F. Khusnutdinova.

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Original Russian Text © E.F. Khusnutdinova, G.N. Apryshko, A.V. Petrova, O.S. Kukovinets, O.B. Kazakova, 2018, published in Bioorganicheskaya Khimiya, 2018, Vol. 44, No. 1, pp. 104–109.

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Khusnutdinova, E.F., Apryshko, G.N., Petrova, A.V. et al. The Synthesis and Selective Cytotoxicity of New Mannich Bases, Derivatives of 19- and 28-Alkynyltriterpenoids. Russ J Bioorg Chem 44, 123–127 (2018). https://doi.org/10.1134/S1068162018010090

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