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

Дьяконов, В.А., Джемилева, Л.У., Туктарова, Р.А., Макаров, А.А., Исламов, И.И., Мулюкова, А.Р., Джемилев, У.М., Dzhemileva, Lilya U., Tuktarova, Regina A., Makarov, Aleksey A., Islamov, Ilgiz I., Mulyukova, Alfiya R., Dzhemilev, Usein 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.

Дьяконов, В.А., Джемилева, Л.У., Туктарова, Р.А., Макаров, А.А., Исламов, И.И., Мулюкова, А.Р., Джемилев, У.М., , , , , , . 2015;
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