ANTITUMOR 2-AMINOCARBONYL-1,2-BIS(METHYLSULFONYL)-1-(SUBSTITUTED)HYDRAZINES

摘要

A compound of the formula: CH3SO2N(Y)N(CONHR)SO2CH3 where Y is -CH3or --CH2CH2Cl; and R is C1-C7 alkyl, cyclohexyl, methylcyclohexyl, -CH2CH=CH2,--CH2CH2Cl, -CH2CH2CH2Cl, -CH2COOC2H5, -CH(CH3)COOC2H5 or -CH(CH2C6H5)COOC2H5.The present invention relates to novel2-aminocarbonyl--1,2-bis(methylsulfonyl)-1-(2-chloroeghyl)hydrazines and2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-methylhydrazines, and their use totreat malignant tumors.The agents are especially useful in the treatment of animal and human cancers.Two preferred agents in this class, especially for use in the treatment oftumors are1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-(2-chloroethyl)aminocarbonylhydrazineand 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-methylaminocarbonylhydrazine.These agents are characterized by the following: They are incapable ofundergoinginactivation by the denitrosation mechanism proposed for the inactivation oftheCNUs roethylation or methylation and carbamoylation.