Microwave accelerated synthesis of isoxazole hydrazide inhibitors of the system xc- transporter: Initial homology model.

Authors :: Matti AA
Mirzaei J
Rudolph J
Smith SA
Newell JL
Patel SA
Braden MR
Bridges RJ
Natale NR
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Nov 01; Vol. 23 (21), pp. 5931-5. Date of Electronic Publication: 2013 Aug 27.
Publication Year :: 2013
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.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Subjects :: 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
Amino Acid Transport System y+ antagonists & inhibitors
Isoxazoles chemistry
Isoxazoles pharmacology

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