1243245-68-2

Upstream product

• 22282-99-1 4-bromo-2-methylpyridine 
• 660867-80-1 2-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine 
• 14062-25-0 Ethyl 4-bromophenylacetate 
• 15250-46-1 ethyl (4-iodophenyl)acetate 

Downstream Products

• 1243245-69-3 2-(4-(2-methylpyridin-4-yl)phenyl)acetic acid 

Relevant academic research and scientific papers

With Wnt signal path to inhibit the active heterocyclic compounds (by machine translation)

The invention relates to a signal path with Wnt inhibiting activity of a heterocyclic compound, including the compound and its pharmaceutically acceptable salt, various isotope, various isomers or various crystal structure, having the general formula I of the structure shown in: the invention relates to a compound and its joint application composition can effectively inhibit the Wnt signal path, can be used for the treatment or prevention of a disorder associated with a Wnt signal path. (by machine translation)

Design, synthesis, and evaluation of potent Wnt signaling inhibitors featuring a fused 3-ring system

The Wnt signaling pathway is a critical developmental pathway which operates through control of cellular functions such as proliferation and differentiation. Aberrant Wnt signaling has been linked to the formation and metastasis of tumors. Porcupine, a member of the membrane-bound O-acyltransferase family of proteins, is an important component of the Wnt pathway. Porcupine catalyzes the palmitoylation of Wnt proteins, a process needed for their secretion and activity. Here we report a novel series of compounds obtained by a scaffold hybridization strategy from a known porcupine inhibitor class. The leading compound 59 demonstrated subnanomolar inhibition of Wnt signaling in a paracrine cellular assay. Compound 59 also showed excellent chemical, plasma and liver microsomal stabilities. Furthermore, compound 59 exhibited good pharmacokinetic profiles with 30% oral bioavailability in rat. Collectively, these results strongly support further optimization of this novel scaffold to develop better Wnt pathway inhibitors.

N- (HETERO)ARYL, 2- (HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS

The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A1, A2, B, Y and Z all represent rings.