76807-59-5

Upstream product

• 76807-53-9 2,4-Dioxo-6-methylpyrido<3,2-d>pyrimidine 5-Oxide 
• 76807-54-0 6-(Acetoxymethyl)-2,4-dioxopyrido<3,2-d>pyrimidine 
• 76807-55-1 6-(Acetoxymethyl)-2,4-dichloropyrido<3,2-d>pyrimidine 
• 76832-40-1 6-(Acetoxymethyl)-4-amino-2-chloropyrido<3,2-d>pyrimidine 
• 76822-61-2 2,4-Diamino-6-(hydroxymethyl)pyrido<3,2-d>pyrimidine 
• 2499-96-9 2,4-Dioxo-6-methylpyrido<3,2-d>pyrimidine 
• 13726-52-8 diethyl N-(p-aminobenzoyl)-L-glutamate 
• 76807-56-2 2,4-diamino-6-(bromomethyl)pyrido<3,2-d>pyrimidine 

Downstream Products

• 76807-63-1 8-Deazaaminopterin 
• 106500-90-7 diethyl N-<4-<<(2,4-diaminopyrido<3,2-d>pyrimidin-6-yl)methyl>propargylamino>benzoyl>-L-glutamate 
• 106500-89-4 N¹⁰-propargyl-8-deazaaminopterin 
• 1955-57-3 6-methylpyrido<3,2-d>pyrimidine-2,4-diamine 
• 939436-99-4 diethyl N-[4-[[2-(2,4-diamino-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-yl)methyl]amino]benzoyl]-L-glutamate 
• 13726-52-8 diethyl N-(p-aminobenzoyl)-L-glutamate 
• 1416159-61-9 N-[4-[(2,4-diaminopyrido[3,2-d]pyrimidin-6-ylmethyl)acetylamino]benzoyl]-L-glutamic acid 
• 1416159-57-3 diethyl N-[4-[2-(2,4-diamino-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-yl methyl)acetylamino]benzoyl]-L-glutamate 
• 1416159-62-0 N-[4-[2-(2,4-diamino-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-ylmethyl)acetylamino] benzoyl]-L-glutamic acid 
• 939437-01-1 diethyl N-[4-[(2-2,4-diamino-5,10-methylene-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-yl methyl)amino]benzoyl]-L-glutamate 
• 939437-02-2 N-[4-[[2-(2,4-Dimino-5,10-methylene-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-yl)methyl] amino]benzoyl]-L-glutamic acid 
• 1416159-60-8 diethyl N-[4-[2-(2,4-diamino-5-formyl-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-yl methyl)acetylamino]benzoyl]-L-glutamate 
• 1416159-64-2 N-[4-[2-(2,4-diamino-5-formyl-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-ylmethyl)acetylamino]benzoyl]-L-glutamic acid 
• 939437-00-0 N-[4-[[2-(2,4-diamino-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-yl)methyl]amino]benzoyl]-L-glutamic acid 

Relevant academic research and scientific papers

Mechanism-based design, synthesis and biological studies of N 5-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and potential anticancer agents

A number of 8-deazatetrahydrofolates bearing electrophilic groups on N 5 were designed and synthesized based on the action mechanism of methionine synthase, and their biological activities were investigated as well. Compounds (11b, 12b and 16)

Novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives as dihydrofolate inhibitor: Design, synthesis and antifolate activity

We report, for the first time, the synthesis and biological activities of 8-deaza-5,6,7,8-tetrahydroaminopterin 9, and the 5-substituted and 5,10-disubstituted analogues 11, 13, 15, and 17. The analogues were obtained from key compound diethyl 8-deaza-5,6,7,8-tetrahydroaminopterin 8 following the catalytic reduction of the pyridine ring of diethyl 8-deaza aminopterin 5. The five novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives were assayed in vitro for their cytotoxicity on BGC-823, HL-60, Bel-7402 and Hela tumor cell lines, and inhibition on recombinant human dihydrofolate reductase (DHFR), among which the most potent molecule (compound 9) was about 4- to 10-fold poorer than MTX on the four kinds of tumor cell lines, and its effect on DHFR was about 17-fold poorer than MTX. The docking studies were followed to explain the biological testing results.

Pyridopyrimidines. 12. Synthesis of 8-deaza analogues of aminopterin and folic acid

A new, general approach to the synthesis of numerous 8-deazafolate and 8-deazaaminopterin analogues is described. The key intermediate, 6-(acetoxymethyl)-2,4-dichloropyrido[3,2-d]pyrimidine, was prepared by chlorination of the 2,4-dioxo derivative which,