1. Microwave accelerated synthesis of isoxazole hydrazide inhibitors of the system xc- transporter: Initial homology model.
- Author
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Matti AA, Mirzaei J, Rudolph J, Smith SA, Newell JL, Patel SA, Braden MR, Bridges RJ, and Natale NR
- 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
- 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., (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Published
- 2013
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