737817-22-0Relevant academic research and scientific papers
2-AMINO-O4-SUBSTITUTED PTERIDINES AND THEIR USE AS INACTIVATORS OF O6-ALKYLGUANINE-DNA ALKYLTRANSFERASE
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Page/Page column 20-21; 1/2, (2008/06/13)
Disclosed are pteridine derivatives of formula (I): (I), wherein, for example, R1 and R2 are hydrogen, C1-C6 alkyl, carboxyl, formyl, C1-C6 hydroxyalkyl, C1-C6 carboxyalkyl, C1-C6 formyl alkyl, C1-C6 alkoxy, acyloxy, acyloxyalkyl wherein the alkyl is C1-C6, halogen, or hydroxy, or a group of formula II: (II); and R3 is (a) phenyl or (b) a cyclic group having at least one 5 or 6-membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fused thereto, wherein each heterocyclic ring has at least one hetero atom chosen from O, N, or S; or (c) a phenyl group or a cyclic group, the cyclic group optionally with a carbocyclic or heterocyclic ring fused thereto, which is substituted with 1 to 5 substituents. Disclosed also are pharmaceutical compositions, a method of enhancing the chemotherapeutic effectiveness of cancer treatment agents, a method of deactivating the O6-alkylguanine-DNA alkyltransferase enzyme, and a method of inhibiting the reaction of O6-alkylguanine-DNA alkyltransferase enzyme with an alkylated DNA.
2-Amino-O4-benzylpteridine derivatives: Potent inactivators of O6-alkylguanine-DNA alkyltransferase
Nelson, Michael E.,Loktionova, Natalia A.,Pegg, Anthony E.,Moschel, Robert C.
, p. 3887 - 3891 (2007/10/03)
2-Amino-O4-benzylpteridine (1), 2-amino-O4-benzyl-6, 7-dimethylpteridine (2), 2-amino-O4-benzyl-6-hydroxymethylpteridine (4), 2-amino-O4-benzylpteridine-6-carboxylic acid (5), 2-amino-O 4-benzyl-6-for
