255874-78-3Relevant academic research and scientific papers
Synthesis and biological evaluation of thiazole derivatives on basic defects underlying cystic fibrosis
Pesce, Emanuela,Pedemonte, Nicoletta,Leoni, Alberto,Locatelli, Alessandra,Morigi, Rita
, (2020)
Cystic fibrosis is a genetic disease caused by loss-of-function mutations in the cystic fibrosis transmembrane conductance regulator gene, encoding for CFTR protein. The most frequent mutation is the deletion of phenylalanine at position 508 (F508del), wh
Discovery of novel dual inhibitors of VEGFR and PI3K kinases containing 2-ureidothiazole scaffold
Li, Lin,Zhang, Cun-Long,Song, Hong-Rui,Tan, Chun-Yan,Ding, Huai-Wei,Jiang, Yu-Yang
, p. 1 - 6 (2016/01/25)
A series of compounds possessing 2-(3-phenyl)ureidothiazol-4-formamide derivatives with a 2-ureidothiazole scaffold were designed and synthesized. Some compounds demonstrated inhibition of cell proliferation against both MDA-MB-231 and HepG2 cell lines using Sorafenib as the positive control. Compounds 6i showed a good to moderate inhibition on VEGFR-2 and PI3Kα which was proved by further molecular docking study. This study suggests that compound 6i is a potential dual inhibitor of VEGFR-2 and PI3Kα and is applicable for further investigation.
Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit
Zbinden, Katrin Groebke,Anselm, Lilli,Banner, David W.,Benz, Joerg,Blasco, Francesca,Decoret, Guillaume,Himber, Jacques,Kuhn, Bernd,Panday, Narendra,Ricklin, Fabienne,Risch, Philippe,Schlatter, Daniel,Stahl, Martin,Thomi, Stefan,Unger, Robert,Haap, Wolfgang
body text, p. 2787 - 2795 (2009/10/17)
Starting from a hit identified by focused screening, 3-aminopyrrolidine factor Xa inhibitors were designed. The binding mode as determined by X-ray structural analysis as well as the pharmacokinetic behaviour of selected compounds is discussed.
Heteroarylacetamide inhibitors of factor Xa
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Page/Page column 6; 14, (2008/06/13)
The invention is concerned with novel heteroarylacetamides of formula (I) [in-line-formulae]Rd—C(O)—N(Re)—Rc—CH2—C(O)—N(Ra)(Rb) ??(I) [/in-line-formulae] wherein Ra to Re /
