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Bioorg Med Chem Lett. 2009 Jan 15;19(2):415-7. doi: 10.1016/j.bmcl.2008.11.057. Epub 2008 Nov 20.

Microwave-assisted one step synthesis of 8-arylmethyl-9H-purin-6-amines.

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  • 1Program in Molecular Pharmacology and Chemistry and Department of Medicine, Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, Box 482, New York, NY 10021, USA.


Molecular chaperone heat shock protein 90 (Hsp90) is an important target in cancer and neurodegenerative diseases, and has rapidly become the focus of several drug discovery efforts. Among small molecule Hsp90 inhibitors with clinical applicability are derivatives of 8-arylmethyl-9H-purin-6-amine class. Here we report the use of microwave-assisted chemistry for the successful one-pot delivery of 8-arylmethyl-9H-purin-6-amines. We discuss the applicability as well as the limitations of this method towards the creation of a large chemical diversity in the 8-arylmethyl-9H-purin-6-amine series.

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