Synthesis, and In Vitro Antitumor Activity of a New Series of 4-Chloro-2-mercapto-5-methylbenzenesulfonamide Derivatives

The synthesis of S-(5-chloro-4-methyl-2-sulfamoylphenyl) N-(phenylsulfonyl)benzothiohydrazonates 4a–k is described. The compounds 4b–f and 4j–k were screened at the US National Cancer Institute for their in vitro activities against a panel of 53–57 human tumor cell lines and relationship between structure and antitumor activity is discussed. The compound 4b was inactive, whereas the remaining compounds exhibited fairly high or reasonable activity (GI50 = 8.12–24.9 miM) against one or more human tumor cell lines.