Evaluation of 2-(methylaminosulfonyl)-1-(arylsulfonyl)hydrazines as anticancer agents

Seven new 2-(methylaminosulfonyl)-1-(arylsulfonyl)hydrazines were prepared and evaluated as potential antitumor agents in vivo against murine Ehrlich ascites carcinoma (EAC). Borderline in vivo activity in EAC was exhibited b y two compounds. All of them were screened in vitro against a battery of hu man tumor cell lines at the National Cancer Institute (NCI), USA. One of th em, namely compound 2f(NSC No. 649 752) displayed highly significant specif icity in two different cell lines as non-small cell lung cancer line HOP-18 and in CNS cancer line SNB-19. The compounds assessed in vitro for anti-HI V activity also at the NCI, however, have not reached the criteria of signi ficant activity. The alkylating activity of the compounds was determined by measuring the absorbance of the alkylated product of 4-(4-nitrobenzyl)pyri dine. It was found that they are capable of acting as chemical alkylating a gents.