90349-87-4Relevant academic research and scientific papers
Design, Synthesis, and Anticancer Activity of New Derivatives of Thiazole and Imidazole
El-Deen,Elsayed,El-Ahwany,El-Azez, M. S. Abd
, p. 2350 - 2355 (2021/02/12)
Abstract: A number of nitrogen heterocyclic derivatives, namely 1,3-thiazole andimidazolidine-2-thione, have been synthesized and their structures confirmed byIR, 1H and 13C NMR, andmass spectra. Cytotoxic activity of some synthesized products has been testedagainst human hepatocellular carcinoma (HepG2) cell line using the MTT assay.The most potent anti-proliferative agent demonstrates activity 2-fold higherthan the reference compound doxorubicin. Three compounds have been characterizedby IC50 value against VEGFR-2. The cell cycle analysis ofcompound 6 has demonstrated cell cycle arrestat G1 phase and accumulation of cells in pre-G1 phase indicating that cytotoxicactivity proceeds via apoptotic pathway.
Discovery and optimization of a highly efficacious class of 5-aryl-2-aminopyridines as FMS-like tyrosine kinase 3 (FLT3) inhibitors
Liu, Gang,Abraham, Sunny,Liu, Xing,Xu, Shimin,Rooks, Allison M.,Nepomuceno, Ron,Dao, Alan,Brigham, Daniel,Gitnick, Dana,Insko, Darren E.,Gardner, Michael F.,Zarrinkar, Patrick P.,Christopher, Ron,Belli, Barbara,Armstrong, Robert C.,Holladay, Mark W.
, p. 3436 - 3441 (2015/08/11)
Based on a putative binding mode of quizartinib (AC220, 1), a potent FMS-like tyrosine kinase 3 (FLT3) inhibitor in Phase III clinical development, we have designed de novo a simpler aminopyridine-based hinge binding motif. Further optimization focusing on maximizing in vivo efficacy and minimizing CYP3A4 time-dependent inhibition resulted in a highly efficacious compound (6s) in tumor xenograft model for further preclinical development.
Design, synthesis and biological evaluation of novel aminothiazoles as antiviral compounds acting against human rhinovirus
Décor, Anne,Grand-Ma?tre, Chantal,Hucke, Oliver,O'Meara, Jeff,Kuhn, Cyrille,Forget, Léa Constantineau,Brochu, Christian,Malenfant, Eric,Bertrand-Laperle, Mégan,Bordeleau, Josée,Ghiro, Elise,Pesant, Marc,Fazal, Gulrez,Gorys, Vida,Little, Michael,Boucher, Colette,Bordeleau, Sylvain,Turcotte, Pascal,Guo, Tim,Garneau, Michel,Spickler, Catherine,Gauthier, Annick
, p. 3841 - 3847 (2013/07/27)
We describe here the design, synthesis and biological evaluation of antiviral compounds acting against human rhinovirus (HRV). A series of aminothiazoles demonstrated pan-activity against the HRV genotypes screened and productive structure-activity relationships. A comprehensive investigational library was designed and performed allowing the identification of potent compounds with lower molecular weight and improved ADME profile. 31d-1, 31d-2, 31f showed good exposures in CD-1 mice. The mechanism of action was discovered to be a host target: the lipid kinase phosphatidylinositol 4-kinase III beta (PI4KIII?). The identification of the pan-HRV active compound 31f combined with a structurally distinct literature compound T-00127-HEV1 allowed the assessment of target related tolerability of inhibiting this kinase for a short period of time in order to prevent HRV replication.
[5,5] sigmatropic shift of N-phenyl-N'-(2-thiazolyl)hydrazines and N,N'- bis(2-thiazolyl)hydrazines into 2-amino-5-(p-aminophenyl)thiazoles and 5,5'- bis(2-aminothiazole) derivatives
Lee, Boong Won,Lee, Seung Dal
, p. 3883 - 3886 (2007/10/03)
[5,5] Sigmatropic shift of N-phenyl-N'-(2-thiazolyl)hydrazines and N,N'- bis(2-thiazolyl)hydrazines in acid-catalyzed benzidine-type rearrangement into 2-amino-5-(p-aminophenyl)thiazoles and 5,5'-bis(2-aminothiazole) derivatives is described, respectively. (C) 2000 Elsevier Science Ltd.
