A novel class of acetylhydrazone derivatives (5a–x) containing 2-(phenylthiomethyl)-1H-benzo-[d]-imidazole moieties are synthesizer, and their antitumor activities against A549, HCT116, HepG2, PC-9, and A375 were determined by the MTT assay. Among them are N-(2,4-dihydroxybenzylidene)-2-(2-(phenylthiomethyl)-1H-benzo[d]-imidazol-1-yl)acetohydrazide (5a) and N-(5-bromo-2-hydroxy-benzylidene)-2-(2-(phenylthiomethyl)-1H-benzo[d]-imidazol-1-yl)acetohydrazide (5d) which displayed excellent cancer inhibitory activity against the tested cancer cells (IC50 4–17 μM), compared with 5-FU and SU11248. The others have moderate to weak inhibitory activity against the tested cancer cell lines.A novel class of acetohydrazide derivatives containing 2-(phenylthiomethyl)-1H-benzo-[d]-imidazole moiety are described, their antitumor activitives against A549, HCT116, HepG2, PC-9, and A375 were determined by the MTT assay. Compounds 5a and 5d displayed excellent cancer inhibitory activity (IC50 4–17 μM).

A series of compounds with a diphenyl ether nucleus were synthesized by incorporating various amines into the diphenyl ether scaffold with an amide bond. Their antitubercular activities were evaluated against Mycobacteriumtuberculosis H37Rv by a microdilution method, with MIC values ranging from 4 to 64 μg/mL. Through structure–activity relationship studies, the two chlorine atoms at 3 and 4 positions in the phenyl ring of R2 group were found to play a significant role in the antitubercular activity. The most potent compound 6c showed an MIC value of 4 μg/mL and a good safety profile in HepG2 cell line by the MTT assay. Compound 6c was further found to be effective in a murine model of BCG infection, providing a good lead for subsequent optimization.A series of compounds with a diphenyl ether nucleus were synthesized and screened for antitubercular activity against Mycobacteriumtuberculosis H37Rv, among which compound 6c was the most potent with MIC value of 4 μg/mL. It was further found to be effective in attenuating the pathological changes caused by BCG infection in vivo.