Design, Synthesis and Anticonvulsant Activity of the Potent Adenosine Kinase Inhibitor GP3269
- 1 July 1997
- journal article
- research article
- Published by Taylor & Francis in Nucleosides and Nucleotides
- Vol. 16 (7-9) , 1013-1021
- https://doi.org/10.1080/07328319708006124
Abstract
The pyrrolopyrimidine nucleoside GP3269 (12) was shown to be a potent and selective inhibitor of human adenosine kinase (IC50 = 11 nM) and to exhibit anticonvulsant activity in rats after oral administration. Synthesis of GP3269 was accomplished in 4 steps from 4-chloro-5-iodopyrrolopyrimidine (9) and the protected 5-deoxy-1-α-chlororibose (8) using a base-catalyzed nucleoside coupling reaction and the Suzuki reaction to replace the 5-iodo substituent with phenyl.Keywords
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