888-79-9Relevant articles and documents
Synthesis and identification of 2,4-bisanilinopyrimidines bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential Aurora A inhibitors
Sang, Chun-Yan,Qin, Wen-Wen,Zhang, Xiu-Juan,Xu, Yu,Ma, You-Zhen,Wang, Xing-Rong,Hui, Ling,Chen, Shi-Wu
, p. 65 - 78 (2018/11/30)
The Aurora kinases are a family of serine/threonine kinases that interact with components of the mitotic apparatus and serve as potential therapeutic targets in oncology. Herein, we reported a series of 2,4-bisanilinopyrimidines bearing 2,2,6,6-tetramethylpiperidine-N-oxyl with selective inhibition of Aurora A in either enzymatic assays or cellular phenotypic assays, and displaying more potent anti-proliferation compared with that of VX-680. The most potent compound 10a forms better interaction with Aurora A than Aurora B in molecular docking. Mechanistic studies revealed that 10a disrupt the spindle formation, block the cell cycle progression in the G2/M phase and induce apoptosis in HeLa cell. These results suggested that the produced series of compounds are potential anticancer agents for further development as selective Aurora A inhibitors.
AMIDO-SUBSTITUTED AZOLE COMPOUNDS
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Page/Page column 63; 64, (2017/05/07)
The present invention relates to compounds of general formula (I), in which X1, X2, R1, R2, R4, R5, R7, and R8 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
Virtual screening and synthesis of new chemical scaffolds as VEGFR-2 kinase inhibitors
Elsayed,El-Araby,Serya,Abouzid
, p. 554 - 560 (2013/02/23)
Background: VEGFR-2 tyrosine kinase inhibitors are currently receiving high interest in drug discovery process as anticancer agents. We have used virtual screening techniques in order to discover new scaffolds that can be used for developing new VEGFR-2 k