101279-39-4Relevant articles and documents
Design, synthesis, and LFA-1/ICAM-1 antagonist activity evaluation of Lifitegrast analogues
An, Yuanlong,Du, Guoxin,Du, Weiwei,Gong, Qi,Hao, Feifei,He, Wei,He, Xiangdong,Jiang, Hualiang,Tong, Xiaochu,Wang, Minnan,Zhang, Donglei,Zheng, Mingyue
, (2022/02/22)
The interaction between Lymphocyte function-associated antigen 1 (LFA-1) and intercellular-adhesion molecule-1 (ICAM-1) plays important roles in the cell-mediated immune response and inflammation associated with dry eye disease. LFA-1/ICAM-1 antagonists can be used for the treatment of dry eye disease, such as Lifitegrast which has been approved by the FDA in 2016 as a new drug for the treatment of dry eye disease. In this study, we designed and synthesized some new structure compounds that are analogues to Lifitegrast, and their biological activities were evaluated by in vitro cell-based assay and also by in vivo mouse dry eye model. Our results demonstrated that one of these analogues of Lifitegrast (compound 1b) showed good LFA-1/ICAM-1 antagonist activity in in vitro assay; meanwhile, it also significantly reduced ocular surface epithelial cells damage, increased goblet cell density in dry eye mouse and highly improved the symptoms of dry eye mouse. [Figure not available: see fulltext.]
CYTOTOXIC PEPTIDES AND ANTIBODY DRUG CONJUGATES THEREOF
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Page/Page column 217, (2013/06/05)
The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.
Design, synthesis, and biological activities of novel 2-cyanoacrylates containing oxazole, oxadiazole, or quinoline moieties
Zhao, Qiqi,Liu, Shaohua,Li, Yonghong,Wang, Qingmin
experimental part, p. 2849 - 2855 (2010/04/30)
A series of novel 2-cyanoacrylates containing an oxazole, oxadiazole, or quinoline moiety were designed and synthesized, and their structures were characterized by 1H NMR and elemental analysis (or high-resolution mass spectrometry). Their herbicidal activities against four weeds were evaluated, and the result indicated that some of the title compounds showed excellent herbicidal activities against rape and amaranth pigweed in postemergence treatment at a dose of 375 g/ha. Furthermore, most of these cyanoacrylates exhibited interesting plant growth regulatory activities.
