207797-05-5Relevant articles and documents
INHIBITOR COMPOUNDS
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Page/Page column 63; 260-261, (2021/01/29)
The disclosure relates to heterocyclic compounds and methods for their preparation. The disclosure provides compounds that may have beneficial therapeutic activity in the treatment of a disease or condition mediated by excessive or otherwise undesirable Des1 and/or fibrotic activity.
Design, synthesis, and evaluation of indeno[2,1-c]pyrazolones for use as inhibitors against hypoxia-inducible factor (HIF)-1 transcriptional activity
Fuse, Shinichiro,Kadonosono, Tetsuya,Kizaka-Kondoh, Shinae,Kuchimaru, Takahiro,Nakamura, Hiroyuki,Sato, Shinichi,Suzuki, Kensuke,Ueda, Hiroki
supporting information, (2019/11/26)
HIF-1 is regarded as a promising target for the drugs used in cancer chemotherapy, and creating readily accessible templates for the development of synthetic drug candidates that could inhibit HIF-1 transcriptional activity is an important pursuit. In this study, indeno[2,1-c]pyrazolones were designed as readily available synthetic inhibitors of HIF-1 transcriptional activity. Nine compounds were synthesized in 4–5 steps from commercially available starting materials. In evaluations of the ability to inhibit the hypoxia-induced transcriptional activity of HIF-1, compound 3c showed a higher level compared with that of known inhibitor, YC-1. The compound 3c suppressed HIF-1α protein accumulation without affecting the levels of HIF-1α mRNA.
Tunable Emission Color of Iridium(III) Complexes with Phenylpyrazole Derivatives as the Main Ligands for Organic Light-Emitting Diodes
Niu, Zhi-Gang,Han, Hua-Bo,Li, Min,Zhao, Zheng,Chen, Guang-Ying,Zheng, You-Xuan,Li, Gao-Nan,Zuo, Jing-Lin
, p. 3154 - 3164 (2018/09/25)
Seven cyclometalated iridium(III) complexes Ir1-Ir7 based on phenylpyrazole derivatives as main ligands and tetraphenylimidodiphosphinate (tpip) as the ancillary ligand were synthesized and fully characterized. The proligands of 1-[4-(trifluoromethyl)phenyl]-1H-pyrazole (cf3ppz, 2a), substituted phenyl-2H-indazole {2-phenyl-2H-indazole (h-1-pidz, 2b), 2-(4-fluorophenyl)-2H-indazole (f-1-pidz, 2c), and 2-[4-(trifluoromethyl)phenyl]-2H-indazole (cf3-1-pidz, 2d)}, and substituted phenyl-1H-indazole {1-phenyl-1H-indazole (h-7-pidz, 2e), 1-(4-fluorophenyl)-1H-indazole (f-7-pidz, 2f), and 1-[4-(trifluoromethyl)phenyl]-1H-indazole (cf3-7-pidz, 2g)} were prepared with good yields. The emission maxima of all Ir(III) complexes can be tuned from 453 to 576 nm with different photoluminescence quantum yields (10.4-70.9%) by varying the type of substituent on the different main ligand frameworks. The organic light-emitting diodes using Ir(III) complexes as the emitters with blue, bluish-green, and yellow colors exhibit a maximum current efficiency and an external quantum efficiency of 39.2 cd A-1 and 14.8%, respectively.