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Synthesis and cytotoxic activities of difluoroacetyl-substituted hexahydropyrimidine derivatives
Journal of Fluorine Chemistry ( IF 1.7 ) Pub Date : 2018-04-22 , DOI: 10.1016/j.jfluchem.2018.04.011
Natalya N. Gibadullina , Dilara R. Latypova , Vener A. Vakhitov , Diana V. Khasanova , Liana F. Zainullina , Yulia V. Vakhitova , Aleksandr N. Lobov , Bogdan I. Ugrak , Yury V. Tomilov , Vladimir A. Dokichev

A series of novel difluoroacetyl hexahydropyrimidine derivatives have been synthesized by reactions of ethyl 4,4-difluoroacetoacetate, 1,1-difluoropentane-2,4-dione and 1,1,5,5-tetrafluoropentane-2,4-dione with an aqueous formaldehyde solution and amino acid ester hydrochlorides under Mannich reaction conditions. The in vitro cytotoxic activity of fluorine-containing hexahydropyrimidine derivatives were determined in cancer (Jurkat and HepG2) and conditionally normal (HEK293) human cells.



中文翻译:

二氟乙酰基取代的六氢嘧啶衍生物的合成及细胞毒活性

通过4,4-二氟乙酰乙酸乙酯,1,1-二氟戊烷-2,4-二酮和1,1,5,5-四氟戊烷-2,4-二酮与水的反应合成了一系列新型的二氟乙酰基六氢嘧啶衍生物。甲醛溶液和氨基酸盐酸盐在曼尼希反应条件下。在体外含氟六氢嘧啶衍生物的细胞毒活性在癌症(Jurkat和HepG2细胞)和正常条件(HEK293)人细胞确定。

更新日期:2018-04-22
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