Type II topoisomerase inhibitor 1

Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area[1][2].

Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

Research Areas >> Infection

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis

Signaling Pathways >> Anti-infection >> Bacterial

topoisomerase IV:0.98 μM (IC50)

DNA gyrase:1.7 nM (IC50)

Type II topoisomerase inhibitor 1 (13 e, 18 h) shows antibacterial activities against E. coli and S. aureus (MIC: 64 and 16 μg/mL, respectively)[1]. .Type II topoisomerase inhibitor 1 (50 μM, 48 h) shows an 8.4% inhibition rate for HepG2 cells[1]. . Cell Viability Assay[1] Cell Line: HepG2 cells Concentration: 10, 50 μM Incubation Time: 10, 50 μM Result: Showed cytoxicity with inhibition rates of 8.4% at 50 μM, 1.5% at 10 μM.

[1]. Fumihito Ushiyama, et al. Lead Identification of 8-(Methylamino)-2-oxo-1,2-dihydroquinoline Derivatives as DNA Gyrase Inhibitors: Hit-to-Lead Generation Involving Thermodynamic Evaluation. ACS Omega. 2020 Apr 24;5(17):10145-10159.

[2]. Fumihito Ushiyama, et al. Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors. Bioorg Med Chem. 2020 Nov 15;28(22):115776.