Abstract
The syntheses of novel tricyclic pyrrolo[2,3-d]pyrimidine analogues of O6–methylguanine and S6–methylthioguanine are described. The crystal structures and pKa values of these analogues are reported. In a standard substrate assay with the human repair protein O6–methylguanine–DNA methyltransferase (MGMT) only the oxygen–containing analogue displayed activity.
Acknowledgments
We are grateful to Dr. Brian Taylor and Ms. Sue Bradshaw for NMR data, Mr. Simon Thorpe for mass spectra. We are also grateful to the EPSRC for financial support.