2-(2-Hydroxyphenyl)-1H-benzimidazole exhibits a multifaceted biological activity profile. It shows moderate to weak inhibition of Co2+-loaded MetAP expressed in _Escherichia coli_, with a 30.37% inhibition at 10 μM and an IC50 value greater than 10000 nM, and also targets MetAP in _Staphylococcus aureus_ and human MetAP2, with inhibition percentages of 66.0%, 12.0%, and 18.0% at 25 μM, respectively. The compound has significant spasmolytic activity in Wistar rat ileum, achieving an Emax of 42.4% and an IC50 of 5150 nM, and a potency index of 1.13 relative to gigantol. 2-(2-Hydroxyphenyl)-1H-benzimidazole inhibits the relaxation of supercoiled plasmid DNA by calf thymus DNA topoisomerase 1 by 95.4% and displays varying levels of cytotoxicity against human A431, HeLa, and MCF7 cells with IC50 values of 30000 nM, 26450 nM, and 16030 nM, respectively, over 72 hours in MTT assays. It also shows antibacterial activity, notably against _Bacillus cereus_ with a MIC of 6.25 μg/mL, and moderate effectiveness against _Pseudomonas aeruginosa_ and _Staphylococcus aureus_ with MIC values of 25.0 μg/mL, but lower activity against other strains like _Salmonella enterica_ and _Escherichia coli_ with MIC values of 400.0 μg/mL. For _Escherichia coli_, it demonstrates an MIC of 25,000 nM, while other strains like _Bacillus cereus_ have MIC values greater than 200,000 nM. The compound shows no cytotoxicity against mouse NIH/3T3 cells (IC50 > 200,000 nM) and moderate antioxidant activity against superoxide radical anions (EC50 122,000 nM), while displaying minimal activity in DPPH radical scavenging (EC50 > 200,000 nM). Additionally, it inhibits human IDO1 activity by 1.0% at 400 μM. Furthermore, antiproliferative activity is observed against human U251MG, IN1528, and IN1760 cells, with EC50 values of 23000 nM, 25000 nM, and 36000 nM, respectively, using the SRB assay over 72 hours..
Note: Summary generated by AI. Data source: ChEMBL 