212621-63-1Relevant articles and documents
Structure-guided identification of novel VEGFR-2 kinase inhibitors via solution phase parallel synthesis
Tripathy, Rabindranath,Reiboldt, Alyssa,Messina, Patricia A.,Iqbal, Mohamed,Singh, Jasbir,Bacon, Edward R.,Angeles, Thelma S.,Yang, Shi X.,Albom, Mark S.,Robinson, Candy,Chang, Hong,Ruggeri, Bruce A.,Mallamo, John P.
, p. 2158 - 2162 (2006)
Structural analysis of the essential binding elements of the oxindole-based kinase inhibitor (1) led to the identification of a novel class of heterocyclic-substituted pyrazolones. Knoevenagel condensation of a variety of activated methylene nucleophiles with indole or pyrrole carboxaldehydes provided a focused library of molecules, each containing elements of kinase pharmacophore probe. Initial screening for VEGFR-2 kinase inhibition eliminated several of the probes. Identification of an active pyrazolone motif and further optimization resulted in several highly potent VEGFR-2 inhibitors with cellular efficacy, anti-angiogenic activity ex vivo in rat aortic ring explant cultures, and oral anti-tumor efficacy in nude mice.
Design and discovery of new pyrimidine coupled nitrogen aromatic rings as chelating groups of JMJD3 inhibitors
Hu, Jianping,Wang, Xin,Chen, Lin,Huang, Min,Tang, Wei,Zuo, Jianping,Liu, Yu-Chih,Shi, Zhe,Liu, Rongfeng,Shen, Jingkang,Xiong, Bing
, p. 721 - 725 (2016)
The histone methylation on lysine residues is one of the most studied post-translational modifications, and its aberrant states have been associated with many human diseases. In 2012, Kruidenier et al. reported GSK-J1 as a selective Jumonji H3K27 demethyl
Phenyl substituted dihydropyridine compound and uses thereof
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Paragraph 0198; 0200-0202, (2019/05/16)
The present invention relates to a phenyl substituted dihydropyridine compound and uses thereof, further to a pharmaceutical composition containing the compound. According to the present invention, the compound or the pharmaceutical composition can be used as mineralocorticoid receptor antagonists.
Histone demethylase JMJD3 inhibitor, preparation method and application thereof
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Paragraph 0114; 0115; 0116, (2017/08/28)
The invention relates to compound shown as general formula (I), its stereoisomer, pharmaceutically acceptable salt, prodrug, solvate, hydrate, ester and crystal. The compound shown as general formula (I) in the invention can inhibit histone demethylase JMJD3, is used for regulating the apparent states of cells and treating a series of histone demethylase JMJD3 mediated diseases and symptoms, which specifically include lung cancer, liver cancer, primary hodgkin lymphoma, some hematologic malignant tumors, inflammation and self-immune diseases, etc.