2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
2-[N'-2-Pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate has been prepared by reaction of chlorambucil with sulfadiazine derivative. Schiffs base has been used as the protective group of the aromatic amine in the synthesis. It can be completely removed by the irradiation of 365 nm UV light at room temperature. The title compound exhibits a high antitumor activity with a therapeutic index (TI) of 47.55 which is twice that of chlorambucil's (TI: 22.84).
Huang
Z
Z
Education Ministry of China, Department of Macromolecular Science, Fudan University, Shanghai. jhuang@fudan.edu.cn
Yang
G
G
Lin
Z
Z
Huang
J
J
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D018906:Antineoplastic Agents, Alkylating / Q000737:chemistry / Q000494:pharmacology; D001557:Benzenesulfonates / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D002699:Chlorambucil / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009368:Neoplasm Transplantation; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D012510:Sarcoma 180 / Q000188:drug therapy; D013411:Sulfadiazine / Q000737:chemistry / Q000494:pharmacology
C436342:2-(N1-2-pyrimidyl-aminobenzenesulfonamido)ethyl 4-bis(2-chloroethyl) aminophenyl butyrate; D000970:Antineoplastic Agents; D018906:Antineoplastic Agents, Alkylating; D001557:Benzenesulfonates; D011743:Pyrimidines; D013411:Sulfadiazine; D002699:Chlorambucil