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JOURNALS // Mendeleev Communications // Archive

Mendeleev Commun., 2019 Volume 29, Issue 2, Pages 163–165 (Mi mendc1457)

This article is cited in 16 papers

Communications

A convenient synthesis of cis-restricted combretastatin analogues with pyrazole and isoxazole cores

D. V. Tsyganova, M. N. Semenovab, L. D. Konyushkina, V. I. Ushkarova, M. M. Raihstata, V. V. Semenova

a N.D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Moscow, Russian Federation
b N.K. Koltsov Institute of Developmental Biology, Russian Academy of Sciences, Moscow, Russian Federation

Abstract: A series of combretastatin analogues, diarylpyrazoles and diarylisoxazoles, have been synthesized and evaluated for their antimitotic tubulin-binding activity using the phenotypic sea urchin (Paracentrotus lividus) embryo assay. One pyrazole analogue and four isoxazole analogues have been identified as potent antimitotic agents comparable with combretastatins A-2 and A-4, with the lowest observable effective concentration of 1–10nmoldm−3 for cleavage alteration of the test embryos.

Language: English

DOI: 10.1016/j.mencom.2019.03.015



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