Xu, Shilin published the artcile1-Phenyl-4-benzoyl-1H-1,2,3-triazoles as Orally Bioavailable Transcriptional Function Suppressors of Estrogen-Related Receptor α, Name: (2-Aminophenyl)(1-(3-isopropylphenyl)-1H-1,2,3-triazol-4-yl)methanone, the publication is Journal of Medicinal Chemistry (2013), 56(11), 4631-4640, database is CAplus and MEDLINE.
Estrogen-related receptor α is a potential candidate target for therapeutic treatment of breast cancer. We describe the discovery and structure-activity relationship study of a series of 1-phenyl-4-benzoyl-1H-1,2,3-triazoles I (R1 = H, OH, F, etc., R2, R3 = H, OH, NH2, R4 = H, iPr, R5 = H, Me, Ph, etc., R6 = H, iPr) and II as novel suppressors of ERRα transcriptional functions. The most promising compound, 2-aminophenyl-(1-(3-isopropylphenyl)-1H-1,2,3-triazol-4-yl)methanone [I (R1 = NH2, R2 = R3 = R4 = R6 = H, R5 = iPr)], potently suppressed the transcriptional functions of ERRα with IC50 = 0.021 μM in a cell-based reporter gene assay and also decreased both the mRNA levels and the protein levels of ERRα and the downstream targets. This compound I (R1 = NH2, R2 = R3 = R4 = R6 = H, R5 = iPr) inhibited the proliferation and migration of breast cancer cells with high level of ERRα. Preliminary pharmacokinetic studies suggested that it possessed a good pharmacokinetic profile with an oral bioavailability of 71.8%. The compounds may serve as novel small mol. probes for further validation of ERRα as a mol. target for anticancer drug development.
Journal of Medicinal Chemistry published new progress about 1437325-71-7. 1437325-71-7 belongs to triazoles, auxiliary class Benzenes, name is (2-Aminophenyl)(1-(3-isopropylphenyl)-1H-1,2,3-triazol-4-yl)methanone, and the molecular formula is C23H20BN, Name: (2-Aminophenyl)(1-(3-isopropylphenyl)-1H-1,2,3-triazol-4-yl)methanone.
Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics