New molecular hybrids containing benzimidazole, thiazolidine-2,4-dione and 1,2,4-oxadiazole as EGFR directing cytotoxic agents was written by Venu, kudapa;Saritha, B.;Sailaja, B. B. V.. And the article was included in Tetrahedron in 2022.Safety of 1-Methyl-1H-benzo[d]imidazole-2-carbaldehyde This article mentions the following:
Herein, some new mol. hybrids having benzimidazole, thiazolidine-2,4-dione and 1,2,4-oxadiazole scaffolds I (Ar = Ph, 3,5-dibromophenyl, 4-pyridyl, etc.) were synthesized from the com. available 1-methyl-1H-benzo[d]imidazole-2-carbaldehyde using two key methodologies such as Knoevenagel condensation and Vilsmeier reagent mediated one-pot synthesis. Further, all the compounds in their μM concentration were screened for their in vitro cytotoxic activity against three human cancer cell lines which includes MCF-7, A-549 and HepG2. Among all, the compound I (Ar = 3,5-dicyanophenyl) exhibited superior activity against all the cell lines as compared to standard drug erlotinib. Besides, the compounds I (Ar = 4-methoxyphenyl, 3,5-dimethoxyphenyl, 4-cyanophenyl) showed superior activity against MCF-7 and most promising activity against A-549 and HepG2 when compared with the pos. control. As well, the tyrosine kinase EGFR inhibitory activity for the potent compounds I (Ar = 4-methoxyphenyl, 3,5-dimethoxyphenyl, 4-cyanophenyl, 3,5-dicyanophenyl), revealed that the compounds I (Ar = 3,5-dimethoxyphenyl, 3,5-dicyanophenyl) displayed nearly double potency as compared to the erlotinib drug. The mol. docking studies of active compounds I (Ar = 4-methoxyphenyl, 3,5-dimethoxyphenyl, 4-cyanophenyl, 3,5-dicyanophenyl) on EGFR target were also conducted and the results were found to be covenant with the corresponding IC50 values. In the experiment, the researchers used many compounds, for example, 1-Methyl-1H-benzo[d]imidazole-2-carbaldehyde (cas: 3012-80-4Safety of 1-Methyl-1H-benzo[d]imidazole-2-carbaldehyde).
1-Methyl-1H-benzo[d]imidazole-2-carbaldehyde (cas: 3012-80-4) belongs to imidazole derivatives. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs. Many drugs contain an imidazole ring, such as certain antifungal drugs, the nitroimidazole series of antibiotics, and the sedative midazolam.Safety of 1-Methyl-1H-benzo[d]imidazole-2-carbaldehyde
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem