The synthesis and properties of tricyclic analogues of S6-methylthioguanine and O6-methylguanine.
Hornillo-Araujo, Ana R ; Burrell, Adam J M ; Aiertza, Miren K ; Shibata, Takayuki ; Hammond, David M ; Edmont, Dolores ; Adams, Harry ; Margison, Geoffrey P ; Williams, David M
Hornillo-Araujo, Ana R
Burrell, Adam J M
Aiertza, Miren K
Shibata, Takayuki
Hammond, David M
Edmont, Dolores
Adams, Harry
Margison, Geoffrey P
Williams, David M
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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.
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Date
2007
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Collections
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Type
Article
Citation
The synthesis and properties of tricyclic analogues of S6-methylthioguanine and O6-methylguanine. 2007, 26 (8-9):1099-102 Nucleosides Nucleotides Nucleic Acids