Dehydrozingerone analogues in synthesis attractive sulfonamide compounds as potential antitumor agents

Abstract

Sulfonamides are very important scaffold in design of different compounds with potential biological activity. They are the basis of several groups of drugs and could be called sulfa drugs. Starting from this fact, we wanted to synthesize some new types of sulfonamides, prepared from derivatives of natural product vanillin. In light of this, we synthesized dehydrozingerone, 4-(4-hydroxy-3-methoxyphenyl)-3-buten-2-one, and its alkyl derivatives. These compounds served as good substrates in the synthesis of new sulfonamide compounds. The structures of the new compounds were determined by IR and NMR methods. Cytotoxicity screening of fourteen new organic compounds against SW480, Hela and MRC-5 was measured by colorimetric MTT assay after 48h of treatment. Cytotoxicity ratio (CR) was calculated as % of cytotoxicity of each compound on normal cells and % of cytotoxicity of the same compounds on tumor cell line. CR is pointed to some new compounds as promising candidates for further experiments.