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Discovery of 5-substituted pyrrolo[2,3-d]pyrimidine antifolates as dual acting inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis: implications of inhibiting 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase to AMPK activation and anti-tumor activity

We synthesized 5-substituted pyrrolo[2,3-d]pyrimidine antifolates (compounds 5–10) with 1 to 6 bridge carbons and a benozyl ring in the side chain as antitumor agents. Compound 8 with a 4-carbon bridge was the most active analog and potently inhibited proliferation of folate receptor (FR) α-expressi...

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Detalhes bibliográficos
Main Authors: Mitchell-Ryan, Shermaine, Wang, Yiqiang, Raghavan, Sudhir, Ravindra, Manasa Punaha, Hales, Eric, Orr, Steven, Cherian, Christina, Hou, Zhanjun, Matherly, Larry H., Gangjee, Aleem
Formato: Artigo
Idioma:Inglês
Publicado em: 2013
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3917155/
https://ncbi.nlm.nih.gov/pubmed/24256410
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm401328u
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