167626-23-5Relevant academic research and scientific papers
A novel NAE/UAE dual inhibitor LP0040 blocks neddylation and ubiquitination leading to growth inhibition and apoptosis of cancer cells
Lu, Peng,Guo, Yahui,Zhu, Lijuan,Xia, Yineng,Zhong, Yuejiao,Wang, Yubin
, p. 294 - 304 (2018)
NEDD8 activating enzyme (NAE) plays an important role in regulating intracellular proteins with key parts in a broad array of cellular functions. On the basis of previously work, a series of 2H-chromen-2-one based NAE inhibitors were designed and synthesized. Through enzyme-based and cell-based assays, LP0040 was identified as a non-nucleoside NAE/UAE dual inhibitor. It could inhibit NAE/UAE activities and downregulated degradations of related substrates in AGS cells, promoting apoptosis in low micromole concentrations. LP0040 possessed anti-proliferation activities with IC50 values of 0.76–3.29 μM against multiple human cancer lines and had synergistic effect with bortezomib. Thus LP0040 represented valuable starting points for future development of NAE/UAE dual inhibitors.
4-substituted pyrido [2, 3-d] pyrimidine-7-ketone compound as well as preparation method and application thereof
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Paragraph 0041-0042; 0056, (2021/05/29)
The invention discloses 4-substituted pyrido [2, 3-d] pyrimidine-7-ketone compounds with different general formula structures and pharmaceutically acceptable salts, solvates, polymorphic substances, tautomers, metabolites or prodrugs of the 4-substituted pyrido [2, 3-d] pyrimidine-7-ketone compounds. The invention also discloses an effect of the compound as an NEDD8 activating enzyme inhibitor and an application of the compound in preparation of drugs for treating diseases related to NEDD8 activating enzyme abnormality. Pharmacological results show that the compound has good NEDD8 inhibitory activity, tumor cell proliferation resistance and tumor cell apoptosis promotion effects.
Coumarin compounds as well as preparation method and application thereof
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Paragraph 0052-0055; 0065, (2021/06/12)
The invention discloses coumarin compounds with different general formula structures and pharmaceutically acceptable salts, solvates, polymorphic substances, tautomers, metabolites or prodrugs thereof. The invention also discloses an effect of the compound as an NEDD8 activating enzyme inhibitor and an application of the compound in preparation of drugs for treating diseases related to NEDD8 activating enzyme abnormality. The invention also discloses an intermediate for preparing the coumarin compound and a preparation method thereof. Pharmacological results show that the compound has high NEDD8 inhibitory activity, tumor cell proliferation resistance and tumor cell apoptosis promotion effects.
Novel selective hindlimb vasodilators: Synthesis and biological activity of 1-acyl-4-aminopiperidine derivatives
Teramoto, Shuji,Tanaka, Michinori,Shimizu, Hiroshi,Fujioka, Takafumi,Tabusa, Fujio,Imaizumi, Takashi,Yoshida, Kenji,Fujiki, Hiroyuki,Mori, Toyoki,Sumida, Takumi,Tominaga, Michiaki
, p. 3033 - 3044 (2007/10/03)
A series of 6-(4-amino-1-piperidinyl)carbonyl-2(1H)-quinolinones, and their open form derivatives, were synthesized and evaluated for their ability to stimulate femoral artery blood flow (FBF) in the canine hindlimb. All members of this series stimulated
