抗肿瘤药物—(Ⅶ)对-氨基苯磺酰胺同型物的合成

Antitumor Compounds-(Ⅶ)Syntheses of Derivatives of Analogues of Sulfanilamide

以对-氨基苯磺酰胺类为载体与植物生长控制剂作用,制备了个7新的对-氨基苯磺酰胺的同型物,通过IR、~1H NMR、MS 的测定,确证它们的化学结构,并初步进行了抗癌试验.

Seven derivatives of plant growth regulators for screening antitumor agentswere synthesized.They are p-(4-chlorophenoxyacetyl-amino)sulfamethazine(Ⅰ),p-(4-Chlorophenoxyacetyl-amino)sulfamethoxazole(Ⅱ),p-(2,4-dichlorophenoxyacety-amino)sulfamethoxazole(Ⅲ),p-(2,4-dichlorophenoxyacetyl-amino)sulfamethoxydiazine(Ⅳ),p-(2,4,5-trichlorophenoxyacetyl-amino)sulfamethazine(Ⅴ),p-(2,3,5-trichloro-benzoyl-amino)sulfamethoxazole(Ⅵ)and p-(2,3,5-trichlorophenzoly-amino)sulfamet-hazine(Ⅶ).Their chemical structures were confirmed by IR,~1HNMR and MS.Preliminary cytotoxicity tests showed that the inhibition ratios of the comp-ounds(100μg/ml)against human cervical cancer Hela cell line in vitro were:85.5%for Ⅰ,71.4% for Ⅱ,88.7% for Ⅲ,53.7% forⅥ,85.4% forⅦ.ⅣandⅤwere notactive.