312723-90-3Relevant academic research and scientific papers
Friedl?nder reaction/quinoxalinone-benzimidazole rearrangement sequence: Expeditious entry to diverse quinoline derivatives with the benzimidazole moieties
Mamedov, Vakhid A.,Kadyrova, Saniya F.,Zhukova, Nataliya A.,Galimullina, Venera R.,Polyancev, Fedor M.,Latypov, Shamil K.
, p. 5934 - 5946 (2015/03/30)
A protocol has been developed for the efficient synthesis of structurally diverse 4-(benzimidazol-2-yl)quinolines via reactions of 3-(2-aminophenyl)quinoxalin-2(1H)-ones and ketones, including acetone, acetophenones, 1,3-pentanedione and ethyl acetoacetat
A potent and selective quinoxalinone-based STK33 inhibitor does not show synthetic lethality in KRAS-dependent cells
We?wer, Michel,Spoonamore, James,Wei, Jingqiang,Guichard, Boris,Ross, Nathan T.,Masson, Kristina,Silkworth, Whitney,Dandapani, Sivaraman,Palmer, Michelle,Scherer, Christina A.,Stern, Andrew M.,Schreiber, Stuart L.,Munoz, Benito
, p. 1034 - 1038 (2013/02/22)
The KRAS oncogene is found in up to 30% of all human tumors. In 2009, RNAi experiments revealed that lowering mRNA levels of a transcript encoding the serine/threonine kinase STK33 was selectively toxic to KRAS-dependent cancer cell lines, suggesting that small-molecule inhibitors of STK33 might selectively target KRAS-dependent cancers. To test this hypothesis, we initiated a high-throughput screen using compounds in the Molecular Libraries Small Molecule Repository (MLSMR). Several hits were identified, and one of these, a quinoxalinone derivative, was optimized. Extensive SAR studies were performed and led to the chemical probe ML281 that showed low nanomolar inhibition of purified recombinant STK33 and a distinct selectivity profile as compared to other STK33 inhibitors that were reported in the course of these studies. Even at the highest concentration tested (10 μM), ML281 had no effect on the viability of KRAS-dependent cancer cells. These results are consistent with other recent reports using small-molecule STK33 inhibitors. Small molecules having different chemical structures and kinase-selectivity profiles are needed to fully understand the role of STK33 in KRAS-dependent cancers. In this regard, ML281 is a valuable addition to small-molecule probes of STK33.
Impact of substituents on the isatin ring on the reaction between isatins with ortho-phenylenediamine
Dowlatabadi, Reza,Khalaj, Ali,Rahimian, Sima,Montazeri, Maedeh,Amini, Mohsen,Shahverdi, Ahmadreza,Mahjub, Elham
experimental part, p. 1650 - 1658 (2011/06/22)
The reaction of different substituted isatins with ortho-phenylenediamine in acetic acid has been investigated. While electron-donor substituents on isatin shift the reaction toward classical 6H-indolo[2,3-b]quinoxaline ring closure, electron-withdrawing
