N. A. Zefirov, Yu. A. Evteeva, A. I. Krasnoperova, A. V. Mamaeva, E. R. Milaeva, S. A. Kuznetsov, O. N. Zefirova, “Tubulin targeted antimitotic agents based on adamantane lead compound: synthesis, SAR and molecular modeling”, Mendeleev Commun., 30:4 (2020), 421

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Mendeleev Communications, 2020, Volume 30, Issue 4, Pages 421–423
DOI: https://doi.org/10.1016/j.mencom.2020.07.005 (Mi mendc1210)

This article is cited in 13 scientific papers (total in 13 papers)

Communications

Tubulin targeted antimitotic agents based on adamantane lead compound: synthesis, SAR and molecular modeling

N. A. Zefirov^ab, Yu. A. Evteeva^a, A. I. Krasnoperova^a, A. V. Mamaeva^a, E. R. Milaeva^ab, S. A. Kuznetsov^c, O. N. Zefirova^ab

^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

Full-text PDF (285 kB) Citations (13) Supplementary materials

DOI: https://doi.org/10.1016/j.mencom.2020.07.005

Graphic abstract: Tubulin targeted antimitotic agents based on adamantane lead compound: synthesis, SAR and molecular modeling

Abstract: 5-Hydroxymethyl-2-methoxyphenyl adamantane-1-acetate inhibits cell proliferation and stimulates depolymerization of microtubules of cancer cells to free tubulin. Its analogues were synthesized via the Steglich or Mitsunobu reactions to determine the role of structural subunits of the molecule in tubulin binding. Based on the structure–activity relationship studies, metabolically stable 1-[2-(5-hydroxymethyl-2-methoxyphenyl)ethyl]adamantane was invented, which exhibits a dual-target profile and retains in vitro activity observed for the lead compound.

Keywords: adamantane, tubulin, colchicine binding site, lung carcinoma A549, dual-target profile, structure–activity relationship.

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Document Type: Article

Language: English

*Supplementary materials:*
		Supplementary_data_1.pdf	(886.9 Kb)

Citation: N. A. Zefirov, Yu. A. Evteeva, A. I. Krasnoperova, A. V. Mamaeva, E. R. Milaeva, S. A. Kuznetsov, O. N. Zefirova, “Tubulin targeted antimitotic agents based on adamantane lead compound: synthesis, SAR and molecular modeling”, Mendeleev Commun., 30:4 (2020), 421–423

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https://www.mathnet.ru/eng/mendc/v30/i4/p421

This publication is cited in the following 13 articles:

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