NOVEL HYBRID MOLECULES ON THE BASIS OF STEROIDS AND (5Z,9Z)-TETRADECA-5,9-DIENOIC ACID: SYNTHESIS, ANTI-CANCER STUDIES AND HUMAN TOPOISOMERASE I INHIBITORY ACTIVITY

D’yakonov, V.A.; Dzhemileva, L.U.; Tuktarova, R.A.; Ishmukhametova, S.R.; Yunusbaeva, M.M.; Ramazanov, I.R.; Dzhemilev, U.M.

NOVEL HYBRID MOLECULES ON THE BASIS OF STEROIDS AND (5Z,9Z)-TETRADECA-5,9-DIENOIC ACID: SYNTHESIS, ANTI-CANCER STUDIES AND HUMAN TOPOISOMERASE I INHIBITORY ACTIVITY

Publication date: 2017

Abstract:

Novel steroid derivatives of 5Z,9Z-dienoic acids were prepared by the DCC/DMAP-catalyzed esterification of (5Z,9Z)-tetradeca-5,9-dienoic acid with hydroxy steroids. High cytotoxicity towards the HEK293, Jurkat, K562 cancer cell lines and human topoisomerase I (hTop1) inhibitory activity in vitro were found for the synthesized acids. A probable mechanism of topoisomerase I inhibition was hypothesized on the basis of in silico studies resorting to docking.

Keywords:
5Z, 9Z-Dienoic acids, steroids, cross-cyclomagnesiation, homogeneous catalysis, 1, 2-dienes, topoisomerase I inhibitors, docking

Тип: Article

DOI: 10.2174/1871520616666161207154850

NOVEL HYBRID MOLECULES ON THE BASIS OF STEROIDS AND (5Z,9Z)-TETRADECA-5,9-DIENOIC ACID: SYNTHESIS, ANTI-CANCER STUDIES AND HUMAN TOPOISOMERASE I INHIBITORY ACTIVITY

Фасеты

Оппонент

Научный руководитель

Авторы

Ключевые слова

Год