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Synthesis and Antitumor Activity of O- and N-Propylamino-Derivatives of Betulin

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Chemistry of Natural Compounds Aims and scope

O- and N-propylamino-derivatives of betulin and betulonic acid oxime and methyl ester were synthesized. Their antitumor activity against a panel of 60 human cancer cell lines was studied. Two betulin derivatives, 3β-hydroxy- 4 and 3β-O-(3-propylamino)-28-O-(3,6-diaminohexyl)lupa-20(29)-ene 5, exhibited antitumor activity against most of 60 cancer cell lines of nine different human tumor types. They were more active than doxorubicin against HCT-15 colon cancer and NCI/ADR-RES ovary cancer cells.

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Acknowledgment

The work was performed on a topic of State Task No. 122031400261-4. We thank the National Cancer Institute for determining the antitumor activity in vitro of 2, 4, 5, 7, 11, 12, 14, and 15.

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Authors and Affiliations

  1. Ufa Institute of Chemistry, Ufa Federal Research Center, Russian Academy of Sciences, 71 Prosp. Oktyabrya, Ufa, 450054, Russia

    G. V. Giniyatullina

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  1. G. V. Giniyatullina
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Correspondence to G. V. Giniyatullina.

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Translated from Khimiya Prirodnykh Soedinenii, No. 4, July–August, 2022, pp. 580–587.

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Giniyatullina, G.V. Synthesis and Antitumor Activity of O- and N-Propylamino-Derivatives of Betulin. Chem Nat Compd 58, 684–692 (2022). https://doi.org/10.1007/s10600-022-03769-9

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  • DOI: https://doi.org/10.1007/s10600-022-03769-9

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