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Anticancer 2-aminocarbonyl-1,2-bis (methylsulfonyl) -1- (substituted) hydrazine

机译:抗癌剂2-氨基羰基-1,2-双(甲磺酰基)-1-(取代)肼

摘要

The present invention relates to novel 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines and 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-methylhydrazines, and their use to treat 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 of tumors are 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-(2-chloroethyl)aminocarbonylhydrazine and 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-methylaminocarbonylhydrazine. These agents are characterized by the following: they are incapable of undergoing inactivation by the denitrosation mechanism proposed for the inactivation of the CNUs; they are incapable of generating a hydroxyethylating species by the mechanism proposed for the CNUs; and they are capable of chloroethylation or methylation and carbamoylation.
机译:本发明涉及新颖的2-氨基羰基-1,2-双(甲基磺酰基)-1-(2-氯乙基)肼和2-氨基羰基-1,2-双(甲基磺酰基)-1-甲基肼,及其在治疗中的用途恶性肿瘤。该试剂在治疗动物和人类癌症中特别有用。特别是用于治疗肿瘤的两种优选的药剂是1,2-双(甲基磺酰基)-1-(2-氯乙基)-2-(2-氯乙基)氨基羰基肼和1,2-双(甲基磺酰基) -1-(2-氯乙基)-2-甲基氨基羰基肼。这些试剂的特征如下:它们不能通过为CNU的失活而提出的脱亚硝化作用而失活;它们不能通过为CNU提出的机制生成羟乙基化物质。它们能够进行氯乙基化或甲基化和氨基甲酰化。

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