Wang, Zhen published the artcileNew ZW4864 Derivatives as Small-Molecule Inhibitors for the β-Catenin/BCL9 Protein-Protein Interaction, Computed Properties of 763120-58-7, the publication is ACS Medicinal Chemistry Letters (2022), 13(5), 865-870, database is CAplus and MEDLINE.
A series of 1-(3-(2-amino-2-oxoethoxy)phenyl)piperidine-3-carboxamide derivatives I [R1 = 2,7-diazaspiro[4.4]nonan-2-ium, 2,7-diazaspiro[4.4]nonan-2-ium, piperazin-1-ium, etc.; R2 = R3 = Me, R2 R3 = -CH2-CH2-, -CH2-CH2-CH2-, etc.], II[R4 = H, Me, iso-Pr, etc.], III[R5 = 3-indolyl, indazol-4-yl, 1H-pyrrolo[2,3-b]pyridin-5-yl, etc.] were reported as new small-mol. β-catenin/B-cell lymphoma 9 (BCL9) protein-protein interaction (PPI) inhibitors. Compounds II were discovered to inhibit the β-catenin/BCL9 PPI with Ki = 0.85-2.7μM. The effects of III[R5 =1H-pyrrolo[2,3-b]pyridin-5-yl] on the β-catenin/BCL9 PPI in cellular context were demonstrated by β-catenin/BCL9 pull-down inhibition and dose-dependent suppression of Wnt/β-catenin signal transactivation. Notably, compound III[R5 =1H-pyrrolo[2,3-b]pyridin-5-yl] is more potent than ZW4864, a previously reported analog, in modulating transcription and expression of β-catenin target genes and suppressing survival of β-catenin-dependent cancer cells. The cellular on-target efficacy of III[R5 =1H-pyrrolo[2,3-b]pyridin-5-yl] was demonstrated by β-catenin rescue experiments Compound III[R5 =1H-pyrrolo[2,3-b]pyridin-5-yl] represents a promising starting point for further optimization of β-catenin/BCL9 PPI inhibitors.
ACS Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C9H6N2O2, Computed Properties of 763120-58-7.
Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics