3-(5-)-Amino-o-diarylisoxazoles: Regioselective synthesis and antitubulin activity

DV Tsyganov, VN Khrustalev, LD Konyushkin…

Index: Tsyganov, Dmitry V.; Khrustalev, Victor N.; Konyushkin, Leonid D.; Raihstat, Mikhail M.; Firgang, Sergei I.; Semenov, Roman V.; Kiselyov, Alex S.; Semenova, Marina N.; Semenov, Victor V. European Journal of Medicinal Chemistry, 2014 , vol. 73, p. 112 - 125

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Citation Number: 6

Abstract

Abstract A regioselective synthesis of both 5-amino-and 3-aminodiarylisoxazoles substituted with polyalkoxyaryl pharmacophores has been validated. Starting materials for the synthetic scheme were easily available from plant extracts. The targeted molecules were further tested in the phenotypic sea urchin embryo assay to identify compounds with antimitotic microtubule destabilizing activity. Structure–activity relationship studies suggested that the ...