E. A. Silyanova, V. I. Ushkarov, A. V. Samet, A. S. Maksimenko, I. A. Koblov, V. P. Kislyi, M. N. Semenova, V. V. Semenov, “A comparative evaluation of monomethoxy substituted <i>o</i>-diarylazoles as antiproliferative microtubule destabilizing agents”, Mendeleev Commun., 2022, Volume 32, Issue 1,Pages <nobr>120

This article is cited in 10 papers

Communications

A comparative evaluation of monomethoxy substituted o-diarylazoles as antiproliferative microtubule destabilizing agents

E. A. Silyanova^a, V. I. Ushkarov^a, A. V. Samet^a, A. S. Maksimenko^a, I. A. Koblov^ab, V. P. Kislyi^a, M. N. Semenova^c, V. V. Semenov^a

^a N.D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Moscow, Russian Federation
^b D.Mendeleev University of Chemical Technology of Russia, Moscow, Russian Federation
^c N.K. Koltsov Institute of Developmental Biology, Russian Academy of Sciences, Moscow, Russian Federation

Abstract: Monomethoxy substituted o-diarylazoles with isoxazole, triazole, pyrazole, or pyrrole linkers were synthesized and evaluated for antimitotic antitubulin activity in a sea urchin embryo model. Structure–activity relationship study revealed that only isoxazole heterocycle together with the unsubstituted phenyl ring next to the heteroatom endowed the molecule with appropriate configuration to exhibit antiproliferative effect by microtubule destabilizing mode of action.

Keywords: o-diarylazoles, nitrostilbenes, triazoles, pyrazoles, isoxazoles, pyrroles, antimitotic activity, microtubule destabilization, sea urchin embryo.

Language: English

DOI: 10.1016/j.mencom.2022.01.039

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