【摘要】 选用l-β-对-甲砜基苯丝氨酸乙酯为载体与植物生长控制剂作用合成了6个新的化合物:l-α-(2,3,5-三氯苯甲酰氨基)-β-(对-甲砜基苯基)丙酸乙酯(Ⅰ),l-α(α’-萘乙酰氨基)-β-(对-甲砜基苯基)丙酸乙酯(Ⅱ),l-α-(β’-萘氧乙酰氨基∫-β-(对-甲砜基苯基)丙酸乙酯(Ⅲ),l-α-(4-氯苯氧乙酰氨基)-β-(对-甲砜基苯基)丙酸乙酯(Ⅳ),l-α-(2,4-二氯苯氧乙酰氨基)-β-(对-甲砜基苯基)丙酸乙酯(Ⅴ)和l-α-(2,4,5-三氯苯氧乙酰氨基)-β-(对-甲砜基苯基)丙酸乙酯(Ⅵ)。试验表明:化合物(浓度100μg/ml)对体外培养的人体子宫颈癌细胞(HeLa细胞)的抑制率,Ⅲ为53.9％,Ⅵ为70.5％,其余不明显。更多还原

【Abstract】 The 1-α-amino-β-hydroxy-β-(p-methylsulfonyl-phenyl)-propyl-ethyl ester was selected as a carrier of plant growth regulators and 6 new derivatives of plant growth regulators were synthesized and screened for antitumor activities: 1-α-(2,3, 5-trichlorobenzoyl-amino)-β-(p-methylsulfonyl-phenyl)-propyl-ethyl ester (Ⅰ), 1-α- (α’- naphthylacetyl-amino)-β-(p-methylsulfonyl-phenyl)-propyl-ethyl ester (Ⅱ), 1-α-(β’-naphthyloxyacetyl-amino)-β-(p-methylsylfonyl-phenyl)-propyl-ethyl ester (Ⅲ), 1-α- (4-chlorophenoxyacetyl-amino) -β-(p-methylsulfonyl-phenyl)-propyl -ethyl ester (Ⅳ), 1-α-(2,4-dichloro-phenoxyacetyl-amino)-β-(p-methylsulfonyl- phenyl)-propyl-ethyl ester (Ⅴ) and 1-α-(2,4,5-trichloro-phenoxyacetyl-amino)-β- (p-methylsulfonyl-phenyl)-propyl-ethyl ester (Ⅵ). Their chemical structures were confirmed by IR, ~1H NMR and MS. Preliminary cytotoxicity tests showed that the inhibition rates of the com- pounds (100μg/ml) against human cervical cancer HeLa cell line in vitro were: 53.9% for compound Ⅲ, 70.5% for compound Ⅵ. Ⅰ, Ⅱ, Ⅳ and Ⅴ were not active.更多还原