D'yakonov Vladimir A, Tuktarova Regina A, Dzhemileva Lilya U, Ishmukhametova Svetlana R, Yunusbaeva Milyausha M, Dzhemilev Usein M
Institute of Petrochemistry and Catalysis of RAS, 141 Prospekt Oktyabrya, 450075 Ufa, Russian Federation.
Institute of Petrochemistry and Catalysis of RAS, 141 Prospekt Oktyabrya, 450075 Ufa, Russian Federation.
Steroids. 2018 Oct;138:14-20. doi: 10.1016/j.steroids.2018.06.002. Epub 2018 Jun 9.
Synthetic analogues of natural 5Z,9Z-dienoic acids - hybrid molecules based on the oximes of cholesterol, pregnenolone, and androsterone with 1,14-tetradeca-5Z,9Z-dienedicarboxylic acid - were synthesized for the first time and studied for antitumor activity in vitro. The acid was prepared using catalytic cyclomagnesiation of O-containing 1,2-dienes with Grignard reagent in the presence of CpTiCl as the key step. Using flow cytometry, it was shown for the first time that the new molecules are efficient apoptosis inducers in the HeLa, Hek293, U937, Jurkat, and K562.
首次合成了天然5Z,9Z - 二烯酸的合成类似物——基于胆固醇、孕烯醇酮和雄甾酮肟与1,14 - 十四碳 - 5Z,9Z - 二烯二羧酸的杂化分子，并对其体外抗肿瘤活性进行了研究。该酸的制备以含O的1,2 - 二烯与格氏试剂在CpTiCl存在下的催化环镁化反应为关键步骤。通过流式细胞术首次表明，这些新分子是HeLa、Hek293、U937、Jurkat和K562细胞中有效的凋亡诱导剂。
