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

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.

SUBMITTER: Matti AA

PROVIDER: S-EPMC3876936 | biostudies-literature | 2013 Nov

REPOSITORIES: biostudies-literature

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

Matti Afnan A AA Mirzaei Joseph J Rudolph John J Smith Stephen A SA Newell Jayme L JL Patel Sarjubhai A SA Braden Michael R MR Bridges Richard J RJ Natale Nicholas R NR

Bioorganic & medicinal chemistry letters 20130827 21

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 ...[more]

PMID: 24042010

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