Design, synthesis, and antitumor screening of certain novel tetrahydroquinoline sulfonamides

Abstract

Sulfonamide containing molecules are of sound biomedical interest. This work comprises the synthesis and in vitro antitumor testing of new library of 20 such molecules. These compounds were screened for cytotoxic activity against three tumor cell lines MCF-7, HeLa, and HepG2 using MTT assay. The yield was low but all the target compounds exhibited antiproliferative activity better than the standard drug Doxorubicin (CAS-23214-92-8). Seven compounds were more potent and four compounds were as active as the standard drug. There were no great difference between compounds obtained from dimedone and those obtained from cyclohexandione. Also no significant difference found in activity between compounds bearing o-amino ethyl ester side chain and compounds bearing o-amino amide derivatives. However, compounds bearing o-amino-cyano group, although retained considerable activity they were far less active than the preceding two. It was clear that monohydroxy aldehyde derivatives were less active compared with the di and trihydroxy ones.

• Antitumor
• sulfonamide
• synthesis
• tetrahydroquinoline

Declaration of interest

This work was supported by a grant from the Graduate Studies and Scientific Research Agency (Grant no. 4.H.33), Salman Bin Abdulaziz University, Alkharj, Saudi Arabia. Thanks are extended to Prof. Dr. Sherif Y. S. Department of Cancer Research, National Cancer Institute, Research Center, Cairo, Egypt, for carrying out the anticancer activities of the tested compounds.