Shen, Hui; Ge, Yiran; Wang, Junwei; Li, Hui; Xu, Yungen; Zhu, Qihua published their research in Bioorganic & Medicinal Chemistry Letters in 2021. The article was titled 《Design, synthesis and biological evaluation of novel molecules as potent PARP-1 inhibitors》.Recommanded Product: 2-Chloro-1H-benzo[d]imidazole The article contains the following contents:
Two series of novel compounds with pthalazin-1(2H)-one moiety such as I [X = N, CH; Y = C(O), CH2; Z = N, CH; R = H, OMe, OEt; R1 = H, C(O)NH2] and 4-(4-fluoro-3-(1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]pyrazine-2-carbonyl)benzyl)phthalazin-1(2H)-one II [R = H, 7-Me, 7-F, 7-Cl] with inhibition activity against PARP-1 were designed and synthesized. All target compounds I and II were evaluated for their PARP-1 inhibition activity and compounds with high PARP-1 inhibition activity were selected to assess for cellular assays in vitro. Among the synthesized compounds compound II [R = 7-F] displayed impressive results in both PARP-1 enzyme inhibition with IC50 value of 0.51 nM and anti-proliferation activity against HCT116 and HCC1937 cell lines with IC50 values of 6.62 nM and 12.65 nM, resp. Also, compound II [R = 7-F] exhibited good metabolic stability in vitro with t1/2 of 173.25 min and CLint of 0.04 mL/min/mg.. Prediction of mol. properties and protein docking were applied to structure design. Prediction of mol. properties and protein docking of compound II [R = 7-F] were applied to structure design. This study provided potential lead compounds and designed the directions for the development of PARP-1 inhibitors. After reading the article, we found that the author used 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Recommanded Product: 2-Chloro-1H-benzo[d]imidazole)
2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1) binds to monoclonal antibodies, inhibiting their binding to their corresponding antigens. This activity may be due to its ability to bind covalently with amino groups on proteins and other molecules.Recommanded Product: 2-Chloro-1H-benzo[d]imidazole
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem