891769-96-3Relevant academic research and scientific papers
The syntheses and properties of tricyclic pyrrolo[2,3-d]pyrimidine 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.
, p. 1723 - 1729 (2008/02/04)
The syntheses of novel tricyclic pyrrolo[2,3-d]pyrimidine analogues of S6-methylthioguanine are described. The crystal structures and pKa values of these and related O6-methylguanine analogues are reported. All compounds display higher pKa values than O 6-methylguanine with the sulfur-containing analogues being the more basic and exhibiting higher stability in aqueous solution. In a standard substrate assay with the human repair protein O6-methylguanine-DNA methyltransferase (MGMT) only the oxygen-containing analogue displayed activity. The Royal Society of Chemistry 2006.
