Ji, Dezhong’s team published research in Bioorganic & Medicinal Chemistry in 2020-03-15 | CAS: 1885-29-6

Bioorganic & Medicinal Chemistry published new progress about Anilines Role: RCT (Reactant), RACT (Reactant or Reagent). 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, SDS of cas: 1885-29-6.

Ji, Dezhong published the artcileDesign, synthesis and biological evaluation of anthranilamide derivatives as potent SMO inhibitors, SDS of cas: 1885-29-6, the main research area is aryl amino benzoyl piperidinyl benzamide preparation antitumor smoothened inhibitor; Anthranilamide; Hedgehog signaling pathway; Molecular dynamics; Ring-opening; Smoothened inhibitor.

A series of anthranilamide derivativesI (R = Ph, 1-methyl-1H-pyrazol-5-yl, 4-phenylpyridine, etc.; R1 = 4-F, 2-CF3-4-F, 4-NO2, etc.; X = N, CH) and II was designed and synthesized as novel smoothened (SMO) inhibitors based on the SMO inhibitor taladegib (LY2940680), which can also inhibit the SMO-D473H mutant, via a ring-opening strategy. The phthalazine core in LY2940680 was replaced with anthranilamide, which retained the inhibitory activity towards the hedgehog (Hh) signaling pathway as evidenced by a dual luciferase reporter gene assay. Compound I (R = Ph; R1 = 2-CF3-4-F; R2 = CH) displayed the best inhibitory activity against the Hh signaling pathway with IC50 value of 34.09 nM, and exhibited better proliferation inhibitory activity towards the Daoy cell line (IC50 = 0.48μM) than LY2940680 (IC50 = 0.79μM).

Bioorganic & Medicinal Chemistry published new progress about Anilines Role: RCT (Reactant), RACT (Reactant or Reagent). 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, SDS of cas: 1885-29-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts