Research paperDesign, synthesis and biological evaluation of 3,4-diaryl-1,2,5-oxadiazole-2/5-oxides as highly potent inhibitors of tubulin polymerization

Add time:08/16/2019    Source:sciencedirect.com

Structure-activity relationships for rigid analogues of combretastatin A-4 (CA-4) were investigated, leading to the discovery of a series of 3,4-diaryl-1,2,5-oxadiazole-N-oxides. Among them, 7n′ and 7n′′ showed remarkable antiproliferative activities against three cancer cell lines in nanomolar concentrations. Interestingly, 7n′ inhibited tubulin polymerization much more efficiently than CA-4. Cellular mechanism investigation elucidated 7n′ disrupted the cellular microtubule structure, arrested cell cycle at G2/M phase and induces apoptosis. Molecular modeling study revealed 1,2,5-oxadiazole-N-oxide ring could increase a hydrogen bond interaction with the binding site. These results provide impetus and further guidance for the development of new CA-4 analogues.

We also recommend Trading Suppliers and Manufacturers of 4-FLUORO-N-(2-[4-(7-HYDROXY-NAPHTHALEN-1-YL)-PIPERAZIN-1-YL]-ETHYL)-BENZAMIDE (cas 135722-26-8). Pls Click Website Link as below: cas 135722-26-8 suppliers

Prev:Synthesis of 4-amino-2-trifluormethyl quinoline derivatives via palladium-catalyzed cascade reactions of isocyanides with N-(ortho-iodo)aryl enamines
Next:Novel 2-(4-methylsulfonylphenyl)pyrimidine derivatives as highly potent and specific COX-2 inhibitors)