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Bioorg Med Chem Lett ; 23(21): 5931-5, 2013 Nov 01.
Article in English | MEDLINE | ID: mdl-24042010

ABSTRACT

Microwave accelerated reaction system (MARS) technology provided a good method to obtain selective and open isoxazole ligands that bind to and inhibit the Sxc- antiporter. The MARS provided numerous advantages, including: shorter time, better yield and higher purity of the product. Of the newly synthesized series of isoxazoles the salicyl hydrazide 6 exhibited the highest level of inhibitory activity in the transport assay. A homology model has been developed to summarize the SAR results to date, and provide a working hypothesis for future studies.


Subject(s)
Amino Acid Transport System y+/antagonists & inhibitors , Isoxazoles/chemistry , Isoxazoles/pharmacology , Amino Acid Transport System y+/chemistry , Amino Acid Transport System y+/metabolism , Cell Line , Cystine/metabolism , Glutamic Acid/metabolism , Humans , Isoxazoles/chemical synthesis , Microwaves , Molecular Docking Simulation , Structural Homology, Protein
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