36729-27-8Relevant articles and documents
Discovery of carbazole carboxamides as novel RORγt inverse agonists
Huang, Yafei,Yu, Mingcheng,Sun, Nannan,Tang, Ting,Yu, Fazhi,Song, Xiaoxia,Xie, Qiong,Fu, Wei,Shao, Liming,Wang, Yonghui
, p. 465 - 476 (2018/02/28)
A novel series of carbazole carboxamides was discovered as potent RORγt inverse agonists using a scaffold hybridization strategy. Structure-activity relationship exploration on the amide linker, carbazole ring and arylsulfone moiety of the hybrid amide 3a led to identification of potent RORγt inverse agonists. Compound 6c was found to have a good RORγt activity with an IC50 of 58.5 nM in FRET assay, and reasonable inhibitory activity in mouse Th17 cell differentiation assay (58.8% inhibition at 0.3 μM). The binding mode of carbazole carboxamides in RORγt ligand binding domain was discussed.
FUNCTIONALISED AND SUBSTITUTED CARBAZOLES AS ANTI-CANCER AGENTS
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Page/Page column 31; 32, (2016/02/26)
The present invention relates to anti-tropomyosin compounds, processes for their preparation, and methods for treating or preventing a disease or disorder, such as a proliferative disease (preferably cancer), using compounds of the invention.
Discovery of ITX 4520: A highly potent orally bioavailable hepatitis C virus entry inhibitor
Mittapalli, Gopi Kumar,Zhao, Fang,Jackson, Andrew,Gao, Hongfeng,Lee, Haekyung,Chow, Stephine,Kaur, Maninder Pal,Nguyen, Natalie,Zamboni, Robert,McKelvy, Jeffrey,Wong-Staal, Flossie,MacDonald, James E.
scheme or table, p. 4955 - 4961 (2012/09/07)
The manuscript reports an identification of a highly potent, orally bioavailable hepatitis C virus entry inhibitor through optimization of a previously reported class of molecules (1) that were not stable in the rat plasma. Compound 39 (ITX 4520) exhibited an excellent PK profile in both rats and dogs with good oral exposure, half-life and oral bioavailability. The compound is also well-tolerated in the preliminary in vivo toxicity studies and has been selected as a pre-clinical candidate for our HCV clinical pipeline.