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

Author

Matti, Afnan A., Mirzaei, Joseph, Rudolph, John, Smith, Stephen A., Newell, Jayme L., Patel, Sarjubhai A., Braden, Michael R., Bridges, Richard J., and Natale, Nicholas R.

Subjects
Molecular Docking Simulation, Amino Acid Transport System y+, Structural Homology, Protein, Cystine, Glutamic Acid, Humans, Isoxazoles, Microwaves, Article, Cell Line
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.

Published
2013

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