Synthesis of some new aryl sulfonyl derivatives and study of their biological activity

This work focuses on the synthesis of some N-aryl sulfonyl derivatives (H1-H9) through the reaction of benzene sulfonyl chloride or P-toluene sulfonyl chloride with aromatic amines containing a pyrimidine ring in their structures (I-VI) in the presence of pyridine as catalyst at room temperature. The spectral data of infrared and nuclear magnetic resonance besides the C, H, N, and S analyses confirmed the validity of the synthesized derivatives. Likewise, the biological activity of the prepared derivatives (H1 - H9) was estimated, including antitumor and antibacterial activity. These activities were determined in vitro using the cytotoxicity assay (MTT cell viability assay) in MCF7 cells to detect the anticancer activity and Kirby-Bauer disc diffusion method used for antibiotic sensitivity test against different pathogenic strains of bacteria. In this study, the MCF-7 cell line was used to assay the anti-proliferative activity of compounds (H1-H9), compound H4 was the most potent in this group with IC50 value of 8.66 μg/mL and compound H8 was the lowest in potency with IC50 value of 52.29 μg/mL. In addition, the synthesized compounds have been screened for antibacterial against six multidrug resistant Gram-positive and Gram-negative bacteria and the results showed effectiveness against tested bacteria.