N. A. Lozinskaya, N. A. Maximova, D. R. Bazanov, S. E. Sosonyuk, B. Wobith, N. A. Zefirov, E. V. Kharitonashvili, O. N. Zefirova, S. A. Kuznetsov, M. V. Proskurnina, “Synthesis and biotesting of new carrier prodrugs of 2-methoxyestradiol”, Mendeleev Commun., 2020, Volume 30, Issue 1,Pages <nobr>7

This article is cited in 3 papers

Communications

Synthesis and biotesting of new carrier prodrugs of 2-methoxyestradiol

N. A. Lozinskaya^ab, N. A. Maximova^a, D. R. Bazanov^a, S. E. Sosonyuk^a, B. Wobith^c, N. A. Zefirov^ab, E. V. Kharitonashvili^a, O. N. Zefirova^ab, S. A. Kuznetsov^c, M. V. Proskurnina^a

^a Department of Chemistry, M.V. Lomonosov Moscow State University, Moscow, Russian Federation
^b Institute of Physiologically Active Compounds, Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Chernogolovka, Moscow Region, Russian Federation
^c Institute of Biological Sciences, Cell Biology and Biosystems Technology, University of Rostock, Rostock, Germany

Abstract: To overcome the metabolic instability of anticancer agent 2-methoxyestradiol, two its dichloroacetylated prodrugs and three new control compounds have been synthesized and evaluated in different in vitro assays with cancer cells A549 and MCF-7. Both prodrugs demonstrated an intrinsic cytotoxicity to A549 cells with no effect on the cellular microtubule network. Molecular modeling has revealed putative weak halogen bond formation of 17-O-dichloroacetylated 2-methoxyestradiol with GTP in the a-tubulin subunit.

Language: English

DOI: 10.1016/j.mencom.2020.01.002

	*Supplementary materials:*
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