329699-54-9Relevant articles and documents
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.
New 2-amino-thiazole-4-acetamides with antiplatelet activity
Rehse, Klaus,Baselt, Tobias
experimental part, p. 645 - 654 (2009/04/06)
In the Born test, 23 title compounds were synthesized and investigated for their antiplatelet activities against collagen, ADP, adrenaline, and platelet-activating factor (PAF) as inducers of the aggregation. Using collagen, three compounds with IC50 values below 10 μM were found (3a, 3b, 3c) and 15 compounds with IC50 values between 10 and 100 μM were determined. In general, a cyclohexylamino rest on an 4-carboxamide moiety is a pre-requisite for this pharmacological activity. A clear dependence from the substituent R1 in the structural element Y is observed. The same is true for the spacer n in the 4-carboxamide substituent. Compound 3e showed strong ADP-antagonistic effects (IC50 = 2.2 nM); 3c antagonized adrenaline (IC50 = 2.8 nM), while 3n was highly effective against platelet-activating factor (IC50 = 0.2 μM).
Heteroarylacetamide inhibitors of factor Xa
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Page/Page column 6; 13-14, (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 /