Disease relevance of NSC 30856

• The binding of p-aminobenzoyl-L-glutamate and 2,4-diaminopyrimidine to dehydrofolate reductase from Lactobacillus casei MTX/R in the presence of a series of co-enzymes and coenzyme analogues has been measured fluorometrically [1].
• In contrast, several 5-substituted 2,4-diaminopyrimidine derivatives markedly inhibited retrovirus replication in cell culture [2].
• Pyrimethamine, a 2,4-diaminopyrimidine useful in the treatment of malaria and toxoplasmosis, was found to enhance antibody and delayed-type hypersensitivity responses to sheep red cells in mice [3].

High impact information on NSC 30856

• 2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists [4].
• We studied 84 dicyclic and tricyclic 2,4-diaminopyrimidine derivatives in this heterologous system and identified those most effective against the DHFR enzymes from each of the pathogens [5].
• Molecular structures of 2,4-diaminopyrimidine antifolates with antineoplastic activity [6].
• Effects of coenzyme analogues on the binding of p-aminobenzoyl-L-glutamate and 2,4-diaminopyrimidine to Lactobacillus casei dihydrofolate reductase [1].
• Selective hydrolysis of 2,4-diaminopyrimidine systems: a theoretical and experimental insight into an old rule [7].

Biological context of NSC 30856

• Four spin-labeled inhibitors of dihydrofolate reductase (DHFR) have been synthesized, each of which has the 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO) reporting group at a different distance from the 2,4-diaminopyrimidine moiety by which the inhibitors are anchored and oriented in the active site [8].
• The structure of the nonclassical pi kappa base pair (7-methyl-oxoformycin B. . .2,4-diaminopyrimidine) was studied at the ab initio Hartree-Fock (HF) and MP2 levels using the 6-31G* and 6-31G** basis sets [9].
• The synthesis and structure-activity relationships of the 4- and 6-substituents of 2,4-diaminopyrimidine-based growth hormone secretagogue receptor (GHS-R) antagonists are described [10].

Gene context of NSC 30856

• The current study examined the effects of etoprine, a highly lipophilic 2,4-diaminopyrimidine that is also a potent DHFR inhibitor, on the fertility of male mice at various dosages (0.1-50 mg/kg/day) for 55 days and male rats at 5 mg/kg/day for 65 days [11].

References