苯乙酰异谷氨酰胺类化合物合成及抗肿瘤活性

The Studies of Syntheses of Phenylacetyl Isoglutamines Derivatives and their antineoplastic activity

苯乙酰异谷酰胺作为抗癌酮 (AntineoplastonA10 )在体内的一种降解产物 ,具有一定程度的抗肿瘤活性。为此设计并合成了一些新的苯乙酰异谷氨酰胺类化合物以测试其抗肿瘤活性。合成中采用在酸性条件下 ,先选择性地对L -谷氨酸γ位羧基进行酯化 ,再进一步合成目标化合物 ,反应条件温和 ,收率好。所合成化合物结构经IR、1HNMR及元素分析鉴定。对所合成的目标化合物的抗肿瘤活性采用MTT法对体外培养的乳腺癌细胞成活率进行了测试 。

As one of degradation products of Antineoplaton A10 in vivo, Phenylacetyl isoglutamine shows some antitumor activities. According to these, we designed and synthesized some novel phenylacetyl isoglutamine derivatives for researching their antitumor activity. In the syntheses of these compounds, in the acid condition, the γ-carboxyl group of L-glutamic acid was selectively transformed to carboxylic ester first, which was then transformed continually to the target molecule. The mild reaction conditions and good yields are the merits of this method. Evaluation of antitumor activity of the target molecules was carried out by MTT method to breast cancer cell strains. The results showed some compounds can inhibit growth of the cancer cells.