185243-93-0Relevant academic research and scientific papers
A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical Probes
Aihara, Hideki,Cui, Huarui,Divakaran, Anand,Ellingson, Mikael O.,Gee, Clifford T.,Griffith, Elizabeth C.,Harki, Daniel A.,Hoell, Zachariah J.,Johnson, Jorden A.,Khanal, Shalil,Lee, Amani L.,Lee, Richard E.,Pomerantz, William C. K.,Scholtz, Cole R.,Shah, Vijay H.,Shi, Ke,Zahid, Huda
supporting information, (2022/01/27)
Chemical probes for epigenetic proteins are essential tools for dissecting the molecular mechanisms for gene regulation and therapeutic development. The bromodomain and extra-terminal (BET) proteins are master transcriptional regulators. Despite promising
Synthesis, characterization and biological activity of bromido[3-ethyl-4-aryl-5-(2-methoxypyridin-5-yl)-1-propyl-1,3-dihydro-2H-imidazol-2-ylidene]gold(i) complexes
Ausserer, Marjana,Baecker, Daniel,Gallati, Caroline M.,Goetzfried, Sina K.,Gust, Ronald,Hermann, Martin,Kircher, Brigitte,Plangger, Matthias,Sagasser, Jessica,Wurst, Klaus
, p. 5471 - 5481 (2020/05/13)
Bromido[3-ethyl-4-aryl-5-(2-methoxypyridin-5-yl)-1-propyl-1,3-dihydro-2H-imidazol-2-ylidene]gold(i) complexes (8a-h) with methoxy, methyl and fluorine substituents at different positions of the 4-aryl ring were synthesized and characterized. The relevance of the 2-methoxypyridin-5-yl residue and the substituents at the 4-aryl ring with regard to the activity against a series of cell lines was determined. Particularly against the Cisplatin-resistant ovarian cancer cell line A2780cis, the most active bromido[3-ethyl-4-(4-methoxyphenyl)-5-(2-methoxypyridin-5-yl)-1-propyl-1,3-dihydro-2H-imidazol-2-ylidene]gold(i) complex8cwas more active than Auranofin. It also inhibited thioredoxin reductase more effectively and induced high amounts of reactive oxygen species in A2780cis cells. Furthermore, its influence on non-cancerous SV 80 lung fibroblasts was lower than that of Auranofin. This fact, together with a high accumulation rate in tumor cells, determined on the example of MCF-7 cells, makes this complex an interesting candidate for further extensive studies.
The base-free van Leusen reaction of cyclic imines on water: Synthesis of N-fused imidazo 6,11-dihydro β-carboline derivatives
Satyam, Killari,Murugesh,Suresh, Surisetti
, p. 5234 - 5238 (2019/06/07)
Construction of imidazoles has been demonstrated on water under base-free conditions. The reaction of dihydro β-carboline imines and p-toluenesulfonylmethyl isocyanides furnished the corresponding substituted N-fused imidazo 6,11-dihydro β-carboline derivatives in very good yields under ambient conditions. The use of deuterium oxide (D2O) as a solvent enabled the incorporation of deuterium isotopes in the imidazole ring.
Organocatalytic asymmetric synthesis of β-aryl-β-isocyano esters
Morana, Fabio,Basso, Andrea,Bella, Marco,Riva, Renata,Banfi, Luca
, p. 2199 - 2210 (2012/11/07)
The asymmetric addition of malonates to in situ generated N-formylimines of aromatic aldehydes was achieved under phase-transfer catalysis using Cinchona alkaloids-derived quaternary ammonium salts. The resulting β- formamidomalonates have been efficientl
An efficient method for the synthesis of substituted TosMIC precursors
Sisko, Joseph,Mellinger, Mark,Sheldrake, Peter W.,Baine, Neil H.
, p. 8113 - 8116 (2007/10/03)
Substituted tosylmethyl isocyanides (TosMICs) are useful reagents for which no general method of preparation is available. We describe here a high-yielding method for the synthesis of substituted tosylmethyl formamides, which are readily converted to the corresponding isocyanides.
