Original article3-(5-)-Amino-o-diarylisoxazoles: Regioselective synthesis and antitubulin activity

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

A regioselective synthesis of both 5-amino- and 3-aminodiarylisoxazoles substituted with polyalkoxyaryl pharmacophores has been validated. Starting materials for the synthetic scheme were easily available from plant extracts. The targeted molecules were further tested in the phenotypic sea urchin embryo assay to identify compounds with antimitotic microtubule destabilizing activity. Structure–activity relationship studies suggested that the structural features essential for potent antiproliferative activity include: 1) 5-aminoisoxazole bridge linking biaryl substituents (rings A and B); 2) unsubstituted 5-amino group; 3) 3,4,5-methoxy substituted benzene and 4-methoxy benzene pharmacophores as rings A and B, respectively. The most potent compounds also showed strong in vitro cytotoxicity in NCI60 anticancer drug screen against a panel of 60 human cancer cell lines, including multi-drug resistant cells.

We also recommend Trading Suppliers and Manufacturers of 3-AMINO-3-(1,3-BENZODIOXOL-5-YL)-1-PROPANOL (cas 113511-45-8). Pls Click Website Link as below: cas 113511-45-8 suppliers

Prev:Chemoenzymatic syntheses of (R)-2-bromo-, (R)2-chloro- and (R)2-azido-1-(1,3-benzodioxol-5-yl)-1-ethanol
Next:A sensitive, direct colorimetric assay of serum zinc using Nitro-paps (cas 113516-70-4) and microwell plates)