N. A. Zefirov, L. Gädert, A. R. Fatkulin, V. M. Shibilev, G. M. Butov, V. M. Mokhov, S. A. Kuznetsov, O. N. Zefirova, “Tubuloclustin analogues with ether moiety: synthesis and evaluation of tubulin clustering and antimitotic activity in cancer cells”, Mendeleev Commun., 30:1 (2020), 106

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Mendeleev Communications, 2020, Volume 30, Issue 1, Pages 106–108
DOI: https://doi.org/10.1016/j.mencom.2020.01.035 (Mi mendc1116)

This article is cited in 10 scientific papers (total in 10 papers)

Communications

Tubuloclustin analogues with ether moiety: synthesis and evaluation of tubulin clustering and antimitotic activity in cancer cells

N. A. Zefirov^ab, L. Gädert^c, A. R. Fatkulin^a, V. M. Shibilev^a, G. M. Butov^d, V. M. Mokhov^e, 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
^d Volzhsky Polytechnic Institute (Branch), Volgograd State Technical University, Volzhsky, Russian Federation
^e Volgograd State Technical University, Volgograd, Russian Federation

Full-text PDF (1771 kB) Citations (10) Supplementary materials

DOI: https://doi.org/10.1016/j.mencom.2020.01.035

Graphic abstract: Tubuloclustin analogues with ether moiety: synthesis and evaluation of tubulin clustering and antimitotic activity in cancer cells

Abstract: New analogues of anticancer agent tubuloclustin N-[7-(adamantan-1-yloxy)-7-heptanoyl]-N-deacetylcolchicine with ether moiety in the linker between colchicine and adamantine fragments were synthesized from w-(adamantan-1-yloxy)alkan- 1-ols. These compounds effectively inhibited growth of human lung carcinoma cell line A549 (IC₅₀=5–15.5nM), induced both apoptosis and formation of tubulin clusters. The conjugates lacking ester carbonyl in the linker exhibit improved metabolic stability and are promising for further cytotoxicity studies in vivo.

Keywords: adamantane, dehydroadamantane, colchicine, tubuloclustin, metabolic stability, tubulin, colchicine binding site, depolymerisation of microtubules, carcinoma A549 cell line..

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Document Type: Article

Language: English

*Supplementary materials:*
		Supplementary_data_1.pdf	(490.1 Kb)

Citation: N. A. Zefirov, L. Gädert, A. R. Fatkulin, V. M. Shibilev, G. M. Butov, V. M. Mokhov, S. A. Kuznetsov, O. N. Zefirova, “Tubuloclustin analogues with ether moiety: synthesis and evaluation of tubulin clustering and antimitotic activity in cancer cells”, Mendeleev Commun., 30:1 (2020), 106–108

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https://www.mathnet.ru/eng/mendc/v30/i1/p106

This publication is cited in the following 10 articles:

Citing articles in Google Scholar: Russian citations, English citations
Related articles in Google Scholar: Russian articles, English articles

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