21117-52-2Relevant academic research and scientific papers
Regioselective nitro group substitution. synthesis of isomeric 4-amino-5-nitro- and 5-amino-4-nitroimidazoles
Zaprutko, Lucjusz,Zwawiak, Justyna,Olender, Dorota,Gzella, Andrzej
, p. 2197 - 2211,15 (2020/08/31)
On the basis of the reactions between 4,5-dinitroimidazole derivatives (1-methyl-4,5-dinitroimidazole, 1,2-dimethyl-4,5-dinitroimidazole and ethyl 2- (4,5-dinitroimidazol-1-yl)acetate) and cyclic amines (morpholine, piperidine or pyrrolidine) in mild cond
ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2
Kiselyov, Alexander S.,Piatnitski, Evgueni L.,Samet, Alexander V.,Kisliy, Victor P.,Semenov, Victor V.
, p. 1369 - 1375 (2007/10/03)
We have developed a series of novel potent ortho-substituted azole derivatives active against kinases VEGFR-1 and VEGFR-2. Both specific and dual ATP-competitive inhibitors of VEGFR-2 were identified. Kinase activity and selectivity could be controlled by varying the arylamido substituents at the azole ring. The most specific molecule (17) displayed >10-fold selectivity for VEGFR-2 over VEGFR-1. Compound activities in enzymatic and cell-based assays were in the range of activities for reported clinical and development candidates (IC50 30 × 10-5 cm/min) is indicative of their potential for intestinal absorption upon oral administration.
