261912-63-4Relevant articles and documents
An alternative modular 'click-SNAr-click' approach to develop subcellular localised fluorescent probes to image mobile Zn2+
Fang, Le,Trigiante, Giuseppe,Crespo-Otero, Rachel,Philpott, Michael P.,Jones, Christopher R.,Watkinson, Michael
, p. 10013 - 10019 (2019)
Zn2+ is involved in a number of biological processes and its wide-ranging roles at the subcellular level, especially in specific organelles, have not yet been fully established due to a lack of tools to image it effectively. We report a new and
An efficient and controlled synthesis of persulfonylated G1 dendrimers: Via click reaction
Khanam, Shaziya,Rai, Sunil K.,Verma, Deepshikha,Khanna, Ranjana S.,Tewari, Ashish K.
, p. 56952 - 56962 (2016/07/06)
This work presents the first report, we believe, on controlled synthesis of clickable dendrimers using aromatic and heteroaromatic cores and persulfonylated dendrons. Owing to poor thermal stability of persulfonylated dendrons, CuAAC reaction conditions w
Fragment-based discovery of novel and selective mPGES-1 inhibitors Part 1: Identification of sulfonamido-1,2,3-triazole-4,5-dicarboxylic acid
Lee, Kijae,Pham, Van Chung,Choi, Min Ji,Kim, Kyung Ju,Lee, Kyung-Tae,Han, Seong-Gu,Yu, Yeon Gyu,Lee, Jae Yeol
, p. 75 - 80 (2013/02/25)
Microsomal prostaglandin E synthase-1 (mPGES-1) is an inducible prostaglandin E synthase that catalyzes the conversion of prostaglandin PGH 2 to PGE2 and represents a novel target for therapeutic treatment of inflammatory disorders. It is essential to identify mPGES-1 inhibitor with novel scaffold as new hit or lead compound for the purpose of the next-generation anti-inflammatory drugs. Herein we report the discovery of sulfonamido-1,2,3-triazole-4,5-dicarboxylic derivatives as a novel class of mPGES-1 inhibitors identified through fragment-based virtual screening and in vitro assays on the inhibitory activity of the actual compounds. 1-[2-(N-Phenylbenzenesulfonamido)ethyl]-1H-1,2,3-triazole-4,5-dicarboxylic acid (6f) inhibits human mPGES-1 (IC50 of 1.1 μM) with high selectivity (ca.1000-fold) over both COX-1 and COX-2 in a cell-free assay. In addition, the activity of compound 6f was again tested at 10 μM concentration in presence of 0.1% Triton X-100 and found to be reduced to 1/4 of its original activity without this detergent. Compared to the complete loss of activity of nuisance inhibitor with the detergent, therefore, compound 6f would be regarded as a partial nuisance inhibitor of mPGES-1 with a novel scaffold for the optimal design of more potent mPGES-1 inhibitors.