Статья

CATALYTIC CYCLOMETALLATION IN STEROID CHEMISTRY III1 : SYNTHESIS OF STEROIDAL DERIVATIVES OF 5Z,9Z-DIENOIC ACID AND INVESTIGATION OF ITS HUMAN TOPOISOMERASE I INHIBITORY ACTIVITY

D’yakonov, V.A., Dzhemileva, L.U., Tuktarova, R.A., Makarov, A.A., Islamov, I.I., Mulyukova, A.R., Dzhemilev, U.M.
2015

Two approaches to stereoselective synthesis of steroid 5Z,9Z-dienoic acids were developed, the first one being based on the cross-cyclomagnesiation of 2-(hepta-5,6-dien-1-yloxy)tetrahydro-2H-pyran and 1,2-diene cholesterol derivatives on treatment with EtMgBr catalyzed by Cp2TiCl2, while the other involving the synthesis of esters of hydroxy steroids with (5Z,9Z)-tetradeca-5,9-dienedioic acid, prepared in two steps using homo-cyclomagnesiation of 2-(hepta-5,6-dien-1-yloxy)tetrahydro-2H-pyran as the key step. High inhibitory activity of the synthesized acids against human topoisomerase I (hTop1) was found.

D’yakonov, V.A., Dzhemileva, L.U., Tuktarova, R.A., Makarov, A.A., Islamov, I.I., Mulyukova, A.R., Dzhemilev, U.M. CATALYTIC CYCLOMETALLATION IN STEROID CHEMISTRY III1 : SYNTHESIS OF STEROIDAL DERIVATIVES OF 5Z,9Z-DIENOIC ACID AND INVESTIGATION OF ITS HUMAN TOPOISOMERASE I INHIBITORY ACTIVITY. 2015;
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