Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. 3034-50-2, formula is C4H4N2O, Name is Imidazole-4-carbaldehyde. The pharmacophore of imidazole exists in bioactive compounds including amino acids, plant growth regulators and therapeutic agents. Formula: C4H4N2O.
Sestito, Simona;Bacci, Andrea;Chiarugi, Sara;Runfola, Massimiliano;Gado, Francesca;Margheritis, Eleonora;Gul, Sheraz;Riveiro, Maria E.;Vazquez, Ramiro;Huguet, Samuel;Manera, Clementina;Rezai, Keyvan;Garau, Gianpiero;Rapposelli, Simona research published 《 Development of potent dual PDK1/AurA kinase inhibitors for cancer therapy: Lead-optimization, structural insights, and ADME-Tox profile》, the research content is summarized as follows. We report the synthesis of novel first-in-class I as dual PDK1-AurA kinase inhibitors as a novel strategy to treat Ewing sarcoma. The most potent compound I [R1 = H, R2 = phenyl] is suitable for progression to in vivo studies. The specific attributes of I [R1 = H, R2 = phenyl] included nanomolar inhibitory potency against both phosphoinositide-dependent kinase-1 (PDK1) and Aurora A (AurA) kinase, with acceptable in vitro ADME-Tox properties (cytotoxicity in 2 healthy and 14 hematol. and solid cancer cell-lines; inhibition of PDE4C1, SIRT7, HDAC4, HDAC6, HDAC8, HDAC9, AurB, CYP1A2, CYP2C9, CYP2C19, CYP2D6, and hERG). X-ray crystallog. and docking studies led to the identification of the key AurA and PDK1/I [R1 = H, R2 = phenyl] interactions. Finally, in vitro drug-intake kinetics and in vivo PK appear to indicate that these compounds are attractive lead-structures for the design and synthesis of PDK1/AurA dual-target mols. to further investigate the in vivo efficacy against Ewing Sarcoma.
Formula: C4H4N2O, 1H-Imidazole-4-carbaldehyde, also known as 1H-Imidazole-4-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%.
The starting material for a practical synthesis of a potent C17,20-lyase inhibitor. The lyase is a key enzyme in androgen biosynthesis as well as a target for treatment of androgen-dependent prostate cancer. Used to synthesize potent antimalarial drug.
1H-Imidazole-4-carbaldehyde is a chemical compound that has been shown to bind to the glucocorticoid receptor. It was synthesized by reacting 1,2-diaminobenzene with formaldehyde and then hydrolyzing the intermediate imidazolium salt, which is stable in acidic solutions. The complex can be prepared by mixing two solutions of imidazole and trifluoroacetic acid. The ligand has a redox potential of -0.1 V (vs NHE). This means it can be oxidized to the carbonyl group or reduced back to the imidazole ring. The compound is stable in neutral solution and forms stable complexes with metal ions such as Cu+, Fe3+, and Zn2+. It also coordinates well with oxygen atoms, nitrogen atoms, and water molecules. 1H-Imidazole-4-carbaldehyde has been shown to bind to glucocortic, 3034-50-2.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem