Substituted Tetrahydronaphthalen‐1‐yl‐phenethyl Ureas: Synthesis, Characterization, and Biological Evaluations

Multi‐target drug discovery is one of the most important objectives in the treatment of carcinogenesis because of the different outcomes of the disease such as bacterial infections due to impaired immune systems. Therefore, a series of new urea derivatives were synthesized to acquire both anti‐proliferative and antimicrobial properties that can be used in chemotherapy. The anti‐cancer and anti‐microbial properties of synthesized urea compounds were investigated on the HeLa cancer line and multiple bacterial strains via using WST‐8 and disc diffusion methods. In anticancer investigations against the HeLa cell line, one synthesized urea derivative exhibited the best activity (IC50: 58.9 μM), which showed up to 8 times less toxic effect (SI: 8.5) against the non‐cancerous human dermal fibroblast (PCS201‐012) cell line. Additionally, some urea derivatives showed antibacterial activities against Acinetobacter baumannii, Escherichia coli, Enterococcus faecalis, and Staphylococcus aureus MRSA with the lowest MIC values. The MIC value obtained against Pseudomonas aeruginosa was at the level of μM for all urea derivatives and was calculated as 7.8125 μM. As a result, some synthesized urea derivatives may be considered as multipotent drug formulations with antibacterial and anticancer properties. N,N′‐dialkylurea derivatives 15–24 were synthesized for the first time and investigated their biological activities against the HeLa cell lines, non‐cancerous cell lines, and some bacterial strains. Especially, compound 21 had anticancer and antibacterial activity in the range of micromolar levels. It had also minimum toxicity profiles against non‐cancerous cell lines. Therefore, it can be considered a multitarget drug in chemotherapeutical applications with its anticancer and antibacterial properties.