944401-56-3Relevant articles and documents
Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives
Chen, Yan-Hong,Ding, Jian,Meng, Ling-Hua,Wang, Yi,Xiang, Hao-Yue,Yang, Chun-Hao,Zhang, Xi
, (2020)
A series of 6-aminocarbonyl pyrrolo[2,1-f][1,2,4]triazine derivatives were designed by scaffold hopping strategy. The IC50 values of compound 14a against PI3Ks were measured, showing selective activity against p110α and p110δ with IC50s of 122 nM and 119 nM respectively. All the synthesized compounds were evaluated for their antiproliferative activity against human cancer cells by SRB assay. Compounds 14a, 14p and 14q exhibited potent antiproliferative activity against five types of human cancer cells and the PK property of 14q was also investigated here.
Oxadiazolopyridine Derivates for Use as Ghrelin O-Acyl Transferase (GOAT) Inhibitors
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Paragraph 0302-0306; 0381-0383, (2018/03/01)
The present invention relates to compounds of general formula I, wherein the groups R1, R2 and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
4-(AZETIDIN-1-YL)PYRIMIDINE DERIVATIVES WITH ANTI-MITOTIC AND ANTI-PROLIFERATIVE ACTIVITY
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Paragraph 0161; 0162, (2017/11/04)
The invention relates to 4-(azetidin-1-yl)pyrimidyl compounds of formula (I), wherein X and Y are, independently of each other CH or N; U is O, CHOH, CHCH2OH, C(CH3)OH, CO, CHNH2; R1 and R2 are, independently of each other H, F or CH3; and R3 is H or CH3; and related compounds with anti-mitotic and anti-proliferative properties, and methods of making use of such compounds in therapy or diagnostics to attenuate undesired cell proliferation, growth, migration, metastasis tumor formation, and inflammatory conditions. Additionally, methods are disclosed of treating diseases associated with undesired angiogenesis and undesired proliferation, and methods of treating infectious and inflammatory diseases using such compounds.