150807-88-8Relevant articles and documents
Design, synthesis, and evaluation of potent Wnt signaling inhibitors featuring a fused 3-ring system
Xu, Zhixiang,Li, Jiajun,Wu, Yiyuan,Sun, Zhijian,Luo, Lusong,Hu, Zhilin,He, Sudan,Zheng, Jiyue,Zhang, Hongjian,Zhang, Xiaohu
, p. 154 - 165 (2015/12/04)
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
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Page/Page column 51-52, (2010/09/18)
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.
Methyl, trifluoromethyl, and methoxycarbonyl - Introduction to the fifth position on the pyridine ring of chloronicotinyl insecticide imidacloprid
Kagabu, Shinzo
, p. 1235 - 1245 (2007/10/03)
Imidacloprid is the first chloronicotinyl insecticide and is currently the largest-selling insecticide worldwide. As a project to find its variants of different insecticidal spectra, derivatives substituted with methyl, trifluoromethyl, and methoxy-carbonyl at the fifth position on the pyridine ring of imidacloprid were prepared. Copyright Taylor & Francis Group, LLC.