TY  - JOUR
T1  - CATALYTIC CYCLOMETALLATION IN STEROID CHEMISTRY III1 : SYNTHESIS OF STEROIDAL DERIVATIVES OF 5Z,9Z-DIENOIC ACID AND INVESTIGATION OF ITS HUMAN TOPOISOMERASE I INHIBITORY ACTIVITY
AU  - D’yakonov, V.A., 
AU  - Dzhemileva, L.U., 
AU  - Tuktarova, R.A., 
AU  - Makarov, A.A., 
AU  - Islamov, I.I., 
AU  - Mulyukova, A.R., 
AU  - Dzhemilev, U.M., 
Y1  - 2018-02-27
UR  - https://repo.bashgmu.ru/publication/674
N2  - 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.