Imidazole based anticancer drug find applications in cancer chemotherapy. 10111-08-7, formula is C4H4N2O, Name is 1H-Imidazole-2-carbaldehyde. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC). Electric Literature of 10111-08-7.
Xu, Yu;Zhang, Xiu-Juan;Li, Wen-Bo;Wang, Xing-Rong;Wang, Shuai;Qiao, Xue-Peng;Chen, Shi-Wu research published 《 Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors》, the research content is summarized as follows. A series of indole-2-one derivatives I (R1 = cyclopropyl, cyclopentyl, 4,5-dihydro-1H-imidazol-2-yl, etc.; R2 = H, Me, cyclopropyl, furan-2-yl; R3 = 4-methoxyphenyl, 2,5-difluorophenyl, naphthalen-1-yl, etc.; R1R2 = -(CH2)3-, -(CH2)5-) and II (R4 = 2-methoxyphenyl, cyclohexyl) through scaffold hopping drug design has been designed and synthesized. Most of the compounds showed potent BRD4 inhibitory activities and anti-proliferation activities in cancer cell lines. Especially, compound I (R1 R2 = -(CH2)3-; R3 = 2-methoxyphenyl) (II) exhibited excellent BRD4 inhibitory activities (BD1 IC50 = 19 nM, BD2 IC50 = 28 nM) and anti-proliferation potency with IC50 values of 4.75μM and 1.35μM in HT-29 and HL-60 cells, resp. Addnl., docking studies showed that the hydrophobic pocket next to KAc region and WPF shelf were critical to the activity of the compound Compound II could arrest the cell-cycle progression of HT-29 cells into the G1 phase and reduce the expression of c-Myc. Moreover, compound II exhibited favorable oral pharmacokinetic properties. All the results demonstrated that compound II was a potent BRD4 inhibitor and had merely potential for colon cancer treatment.
10111-08-7, 1H-Imidazole-2-carbaldehyde, also known as 1H-Imidazole-2-carbaldehyde, is a useful research compound. Its molecular formula is C4H4N2O and its molecular weight is 96.09 g/mol. The purity is usually 95%.
1H-Imidazole-2-carboxaldehyde is a novel PTP1b inhibitor with potential application to treat type 2 diabetes.
1H-Imidazole-2-carboxaldehyde is a broad-spectrum antimicrobial that has been shown to inhibit the growth of bacteria by interfering with protein synthesis. It binds to the cytosolic protein and receptor molecule, which are involved in the activation of bacterial enzymes. Imidazole-2-carboxaldehyde reacts with anhydrous sodium and copper complex to produce hydrogen bonds, which prevent the formation of the nitrogen atoms necessary for cellular processes. This chemical also has biological properties such as glyoxal, which inhibits bacterial growth by reacting with amino groups on proteins., Electric Literature of 10111-08-7
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem