Imidazole Biochem/physiol Actions: Imidazole derivatives have antibacterial, antifungal and anticancer functionality. It interacts with DNA and also binds to protein and stops cell division. 3034-50-2, formula is C4H4N2O, Name is Imidazole-4-carbaldehyde. It also acts as a microtubule destabilizing agents and inhibits topoisomerase and Cytochrome P450 Family 26 Subfamily A Member 1 (CYP26A1) enzymes. Quality Control of 3034-50-2.
Caciolla, Jessica;Martini, Silvia;Spinello, Angelo;Pavlin, Matic;Turrini, Eleonora;Simonelli, Federica;Belluti, Federica;Rampa, Angela;Bisi, Alessandra;Fimognari, Carmela;Zaffaroni, Nadia;Gobbi, Silvia;Magistrato, Alessandra research published 《 Balanced dual acting compounds targeting aromatase and estrogen receptor α as an emerging therapeutic opportunity to counteract estrogen responsive breast cancer》, the research content is summarized as follows. Breast Cancer (BC) is a leading cause of death in women, currently affecting 13% of female population worldwide. First-line clin. treatments against Estrogen Receptor pos. (ER+) BC rely on suppressing estrogen production, by inhibiting the aromatase (AR) enzyme, or on blocking estrogen-dependent pro-oncogenic signaling, by targeting Estrogen Receptor (ER) α with selective Modulators/Degraders (SERMs/SERDs). The development of dual acting mols. targeting AR and ERα represents a tantalizing alternative strategy to fight ER + BC, reducing the incidence of adverse effects and resistance onset that limit the effectiveness of these gold-standard therapies. Here, in silico design, synthesis, biol. evaluation and an at.-level characterization of the binding and inhibition mechanism of twelve structurally related drug-candidates enable the discovery of multiple compounds active on both AR and ERα in the sub-μM range. The best drug-candidate 3a displayed a balanced low-nanomolar IC50 towards the two targets, SERM activity and moderate selectivity towards a BC cell line. Moreover, most of the studied compounds reduced ERα levels, suggesting a potential SERD activity. This study dissects the key structural traits needed to obtain optimal dual acting drug-candidates, showing that multitarget compounds may be a viable therapeutic option to counteract ER + BC.
3034-50-2, 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, Quality Control of 3034-50-2
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem