防癌药物的研究——维生素甲酸衍生物的合成
STUDIES ON COMPOUNDS OF TUMOR PREVENTION—— SYNTHESIS OF DERIVATIVES OF RETINOICACID
-
摘要: 为寻找防癌药物,从改变维甲酸的结构、物化性质,以改变在体内的运转、分布和生物活性,达到提高疗效,降低毒性的目的,而合成了27个维甲酸酯和酰胺衍生物。部分化合物已进行预防致癌实验。结果证明,有些化合物有效,其中维甲酰(4-乙氧羰基苯胺)(1)的效果较好,毒性低,可能是一个有希望的防癌化合物。Abstract: In search of agents for tumor prevention, attempt to improve the biological activity of the parent compound, retinoic acid, was carried out by preparing its esters and amides through which the physical and chemical properties and pharmacodynamics might be changed. Twenty-seven retinoic acid esters and retinamides were prepared by treating the corresponding amine and alcohol with retinyl chloride which was obtained from retinoic acid and phosphorous trichloride. Animal tests of part of the compounds reported in this paper showed that some of them exhibited preventive activity against carcinogenic action of nitrososarcosine among which compound (1), N-(4-ethoxycarbophenyl) retinamide showed higher activity and lower toxicity.
下载: