Certain 8-amino-9-(benzyl)guanines as potential purine nucleoside phosphorylase inhibitors
dc.contributor.author | Chem, J. W. | en_US |
dc.contributor.author | Wise, Dean S. | en_US |
dc.contributor.author | Shewach, Donna S. | en_US |
dc.contributor.author | Daddona, Peter E. | en_US |
dc.contributor.author | Townsend, Leroy B. | en_US |
dc.date.accessioned | 2006-04-10T18:24:27Z | |
dc.date.available | 2006-04-10T18:24:27Z | |
dc.date.issued | 1994 | en_US |
dc.identifier.citation | Chem, JW, Wise, DS, Shewach, DS, Daddona, PE, Townsend, LB (1994)."Certain 8-amino-9-(benzyl)guanines as potential purine nucleoside phosphorylase inhibitors." European Journal of Medicinal Chemistry 29(1): 3-9. <http://hdl.handle.net/2027.42/31845> | en_US |
dc.identifier.uri | http://www.sciencedirect.com/science/article/B6VKY-4C9YYM5-VX/2/188d6087ddccc785df99f577a3a60f99 | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/31845 | |
dc.description.abstract | Several 8-amino-9-(benzyl)guanines were selected for synthesis as potential purine nucleoside phosphorylase (PNP) inhibitors on the basis of the Topliss decision tree. These compounds were prepared by the treatment of oxazolo[5,4-d]pyrimidine intermediates with potassium carbonate in a 1-pot reaction. All compounds were evaluated for PNP inhibitory activity using an in vitro enzyme inhibition assay. The extent of binding to PNP appeared to be influenced by the presence of electron donating substituents on the phenyl ring of the benzyl group. None of the tested compounds were more active than the parent compound, 8-amino-9-benzylguanine. The inhibitory activity seems to be most likely -[sigma]-dependent. | en_US |
dc.format.extent | 866870 bytes | |
dc.format.extent | 3118 bytes | |
dc.format.mimetype | application/pdf | |
dc.format.mimetype | text/plain | |
dc.language.iso | en_US | |
dc.publisher | Elsevier | en_US |
dc.title | Certain 8-amino-9-(benzyl)guanines as potential purine nucleoside phosphorylase inhibitors | en_US |
dc.type | Article | en_US |
dc.rights.robots | IndexNoFollow | en_US |
dc.subject.hlbsecondlevel | Chemistry | en_US |
dc.subject.hlbsecondlevel | Chemical Engineering | en_US |
dc.subject.hlbsecondlevel | Biological Chemistry | en_US |
dc.subject.hlbtoplevel | Engineering | en_US |
dc.subject.hlbtoplevel | Science | en_US |
dc.subject.hlbtoplevel | Health Sciences | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | Department of Biological Chemistry, University of Michigan, Ann Arbor, MI, USA; Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI, USA. | en_US |
dc.contributor.affiliationum | Department of Biological Chemistry, University of Michigan, Ann Arbor, MI, USA; Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI, USA. | en_US |
dc.contributor.affiliationum | Department of Chemistry, University of Michigan, Ann Arbor, MI, USA | en_US |
dc.contributor.affiliationum | Department of Internal Medicine, University of Michigan, Ann Arbor, MI, USA | en_US |
dc.contributor.affiliationum | Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, MI, USA | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/31845/1/0000793.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1016/0223-5234(94)90119-8 | en_US |
dc.identifier.source | European Journal of Medicinal Chemistry | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
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