1214381-00-6Relevant articles and documents
Synthesis of biscyclometalated iridium(III) acetylacetonate complexes via a 15 min bridge-splitting reaction, their characterisations and photophysical properties
Alt?n?l?ek, Nuray,Aydemir, Murat,Tavasl?, Mustafa,Dos Santos, Paloma L.,Monkman, Andrew P.
, p. 184 - 188 (2017)
Chloro-bridged diiridium(III) complexes (4a and 4b) were subjected to a bridge-splitting reaction with acetylacetone and sodium carbonate in 2-ethoxyethanol. The reaction was complete within 15 min and two novel biscyclometalated iridium(III) acetylaceton
Synthesis and evaluation of the HIF-1α inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5
Jiang, Zhe,Jin, Cheng Hua,Jin, Xuejun,Li, Shanji,Li, Xiang-Yu,Li, Yan-Wei,Ma, Juan,Piao, Hu-Ri,Zhao, Li-Min
, (2019)
The transcription factor hypoxia-inducible factor-1α (HIF-1α) plays an important role in apoptosis, metastasis, and proliferation and is recognized as an important potential therapeutic target for cancer. Six series of 3(5)-(6-methylpyridin-2-yl)-4-(quinolin-4-yl)pyrazoles (11a–d, 12a–d, and 18a–d) and 3(5)-(6-methylpyridin-2-yl)-4-(2-phenyl-pyridin-4-yl)pyrazoles (19a–d, 20a–d, and 21a–d) were synthesized and evaluated for activin receptor-like kinase 5 (ALK5) and HIF-1α inhibitory activity at the enzyme and cell levels. The effect of the lead compound 20d (J-1012) on HIF-1α activation in HCT116 cells was investigated. J-1012 markedly decreased the hypoxia-induced or TNF-induced accumulation of HIF-1α protein dose-dependently. Analysis revealed that J-1012 inhibited HIF-1α protein synthesis, without affecting the degradation of HIF-1α protein. Furthermore, by inhibiting the activation of HIF-1α, J-1012 suppressed the metastasis and proliferation and promoted apoptosis of HCT116 cells. These results suggest that J-1012 may be a potential therapeutic agent against human colon cancer.
ALKOXYBENZO-FIVE-MEMBERED (SIX-MEMBERED) HETEROCYCLIC AMINE COMPOUND AND PHARMACEUTICAL USE THEREOF
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Paragraph 0118-0120, (2020/12/22)
The invention relates to alkoxybenzeno five- or six-member heterocyclic amines compounds as scheme I , in which the R1, R2 and R3 are consistent with the detailed description in the patent claim. The compounds can act as selective sphingomyelin synthase 2 (SMS2) inhibitors to treat diseases caused by abnormal increasing of sphingomyelin (SM). This invention also includes compounds as scheme I , including pharmaceutically acceptable salts, pharmaceutical compositions as the active ingredients, and their application in drugs which can prevent and cure diseases caused by abnormal increasing of SM. These diseases caused by abnormal increasing of SM include atherosclerosis, type II diabetes, fatty liver, obesity, metabolic syndromes, enteritis and other inflammatory diseases.
ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
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Paragraph 0128; 0129, (2019/12/06)
A neutral compound including a first ligand LA represented by Formula I or Formula II is disclosed.