The synthesis and properties of tricyclic analogues of S6-methylthioguanine and O6-methylguanine.
dc.contributor.author | Hornillo-Araujo, Ana R | |
dc.contributor.author | Burrell, Adam J M | |
dc.contributor.author | Aiertza, Miren K | |
dc.contributor.author | Shibata, Takayuki | |
dc.contributor.author | Hammond, David M | |
dc.contributor.author | Edmont, Dolores | |
dc.contributor.author | Adams, Harry | |
dc.contributor.author | Margison, Geoffrey P | |
dc.contributor.author | Williams, David M | |
dc.date.accessioned | 2009-06-23T15:44:49Z | |
dc.date.available | 2009-06-23T15:44:49Z | |
dc.date.issued | 2007 | |
dc.identifier.citation | The synthesis and properties of tricyclic analogues of S6-methylthioguanine and O6-methylguanine. 2007, 26 (8-9):1099-102 Nucleosides Nucleotides Nucleic Acids | en |
dc.identifier.issn | 1525-7770 | |
dc.identifier.pmid | 18058544 | |
dc.identifier.doi | 10.1080/15257770701519221 | |
dc.identifier.uri | http://hdl.handle.net/10541/71361 | |
dc.description.abstract | The syntheses of novel tricyclic pyrrolo[2,3-d]pyrimidine analogues of O(6)-methylguanine and S(6)-methylthioguanine are described. The crystal structures and pK(a) values of these analogues are reported. In a standard substrate assay with the human repair protein O(6)-methylguanine-DNA methyltransferase (MGMT) only the oxygen-containing analogue displayed activity. | |
dc.language.iso | en | en |
dc.subject.mesh | Crystallography, X-Ray | |
dc.subject.mesh | Drug Design | |
dc.subject.mesh | Enzyme Inhibitors | |
dc.subject.mesh | Guanine | |
dc.subject.mesh | Humans | |
dc.subject.mesh | Kinetics | |
dc.subject.mesh | Molecular Structure | |
dc.subject.mesh | O(6)-Methylguanine-DNA Methyltransferase | |
dc.title | The synthesis and properties of tricyclic analogues of S6-methylthioguanine and O6-methylguanine. | en |
dc.type | Article | en |
dc.contributor.department | Centre for Chemical Biology, Department of Chemistry, University of Sheffield, Sheffield, United Kingdom. | en |
dc.identifier.journal | Nucleosides, Nucleotides & Nucleic Acids | en |
html.description.abstract | The syntheses of novel tricyclic pyrrolo[2,3-d]pyrimidine analogues of O(6)-methylguanine and S(6)-methylthioguanine are described. The crystal structures and pK(a) values of these analogues are reported. In a standard substrate assay with the human repair protein O(6)-methylguanine-DNA methyltransferase (MGMT) only the oxygen-containing analogue displayed activity. |