6-(p-Hydroxyphenylhydrazino)uracil (H2-HPUra) is a selective and potent inhibitor of the replication-specific class III DNA polymerase (pol III) of Gr+ bacteria. Although formally a pyrimidine, H2-HPUra derives its inhibitory activity from its specific capacity to mimic the purine nucleotide, dGTP. We
The Journal of organic chemistry, 69(9), 3212-3215 (2004-04-24)
A convergent synthesis of adenosine A2a agonist 1 in the form of its maleate salt 2 was achieved. The key step in this approach was the highly selective 9beta-glycosylation reaction between 2-haloadenines or an N(2)-alkyl-6-chloroguanine and a D-ribose derivative containing
Journal of medicinal chemistry, 48(11), 3919-3929 (2005-05-27)
Derivatives of the herpes simplex thymidine kinase inhibitor HBPG [2-phenylamino-9-(4-hydroxybutyl)-6-oxopurine] have been synthesized and tested for inhibitory activity against recombinant enzymes (TK) from herpes simplex types 1 and 2 (HSV-1, HSV-2). The compounds inhibited phosphorylation of [3H]thymidine by both enzymes
Chemical research in toxicology, 11(12), 1453-1459 (1998-12-22)
2-Nitropropane, an industrial chemical and a hepatocarcinogen in rats, induces aryl sulfotransferase-mediated liver DNA and RNA base modifications [Sodum, R. S., Sohn, O. S., Nie, G., and Fiala, E. S. (1994) Chem. Res. Toxicol. 7, 344-351]. Two of these modifications
Journal of combinatorial chemistry, 4(2), 183-186 (2002-03-12)
A resin-capture and release strategy for making combinatorial 2,6,9-trisubstituted purine libraries is demonstrated by capturing N9-derivatized purines at the C6 position with a thio-modified polymer. The C2 fluoro group is subsequently substituted with primary and secondary amines followed by thioether
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