AHPA衍生物的设计、合成及抗癌活性研究

Design,synthesis and anti-cancer activityof AHPA derivatives

目的以基质金属蛋白酶AP N为靶点 ,寻找新的抗癌活性化合物。方法以 3 氨基 2 羟基 4 苯基丁酸 亮氨酸 (AHPA Leu)为先导化合物 ,借助计算机分子结构优化处理进行合理药物设计 ,合成了 8个结构全新的AHPA衍生物 ,并对目标化合物进行了体内、体外初步药效学评价。结果与结论初步药效学评价表明 ,所合成的化合物能增强小鼠的免疫功能 ,抑制S1 80 肿瘤生长 。

Aim To discover new active compounds against the cancer a targeted on AP N.Methods The paper focused on 3 amino 2 hydroxy 4 phenyl butanoic acid leucine(AHPA Leu)as a lead compound,eight APHA derivatives were designed and synthesized.The preliminary pharmacodynamic evaluations in vitro and in vivo of these compounds were also carried out.Results and Conclusion The preliminary pharmacodynamic evaluation suggests that these compounds can promote immunology function of mice and inhibit the growth of S 180 tumor.The compound Ⅵ shows the most potent activity.