Abstract

The reaction of ethyl benzoylacetate with formaldehyde and natural amino acid ester hydrochlorides in acetate buffer (AcONa/AcOH, pH 4.0) at room temperature afforded 41–61% of new 5-benzoylhexahydropyrimidine derivatives. The synthesized compounds were evaluated for their in vitro cytotoxic activity against normal (HEK293) and tumor cell lines (Jurkat, HepG2). T-Lymphoblastic leukemia Jurkat cells turned out to be most sensitive to the examined hexahydropyrimidine derivatives. Ethyl 5-benzoyl-1,3-bis[2-ethoxy-1-(4-hydroxybenzyl)-2-oxoethyl]hexahydropyrimidine-5-carboxylate showed the highest cytotoxic activity against all tested cell lines.

中文翻译：

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5-苯甲酰六氢嘧啶衍生物的合成及细胞毒活性

摘要

在室温下，苯甲酰乙酸乙酯与甲醛和天然氨基酸酯盐酸盐在乙酸盐缓冲液（AcONa/AcOH，pH 4.0）中反应，得到 41-61% 的新 5-苯甲酰六氢嘧啶衍生物。评估合成的化合物对正常细胞系 (HEK293) 和肿瘤细胞系 (Jurkat, HepG2) 的体外细胞毒活性。T-淋巴细胞白血病 Jurkat 细胞对所检测的六氢嘧啶衍生物最为敏感。Ethyl 5-benzoyl-1,3-bis[2-ethoxy-1-(4-hydroxybenzyl)-2-oxoethyl]hexahydropyrimidine-5-carboxylate 对所有测试的细胞系显示出最高的细胞毒活性。