4282-46-6Relevant articles and documents
S-triazine compounds as well as preparation method and application thereof
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Paragraph 0104-0106, (2020/05/05)
The invention discloses s-triazine compounds and pharmaceutically acceptable salts thereof; experiments prove that the compounds can be used for treating or preventing diseases related to protein kinase activity, such as leukemia and lymphoma, by inhibiti
Synthesis method of 3-(4-nitrophenyl)pyridine
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Paragraph 0027; 0028; 0029; 0030; 0031; 0032; 0033-0113, (2019/02/04)
The invention relates to a synthesis method of 3-(4-nitrophenyl)pyridine. The synthesis method of the 3-(4-nitrophenyl)pyridine comprises the following steps: S1, under the protection of inert gas, mixing 4-nitrophenylboronic acid, 3-chloropyridine, n-het
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.