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ЖУРНАЛЫ // Mendeleev Communications // Архив

Mendeleev Commun., 2022, том 32, выпуск 1, страницы 120–122 (Mi mendc591)

Эта публикация цитируется в 10 статьях

Communications

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

E. A. Silyanovaa, V. I. Ushkarova, A. V. Sameta, A. S. Maksimenkoa, I. A. Koblovab, V. P. Kislyia, M. N. Semenovac, V. V. Semenova

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


Аннотация: 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.

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

Язык публикации: английский

DOI: 10.1016/j.mencom.2022.01.039



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