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Synthesis and biological activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier for cellular entry(†)

2-Amino-4-oxo-6-substituted pyrrolo[2,3-d]pyrimidines with a thienoyl side chain and 4-6 carbon bridge lengths (compounds 1-3) were synthesized as substrates for folate receptors (FRs) and the proton-coupled folate transporter (PCFT). Conversion of acetylene carboxylic acids to α-bromomethylketones...

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Main Authors: Wang, Lei, Cherian, Christina, Desmoulin, Sita Kugel, Polin, Lisa, Deng, Yijun, Wu, Jianmei, Hou, Zhanjun, White, Kathryn, Kushner, Juiwanna, Matherly, Larry H., Gangjee, Aleem
Formato: Artigo
Idioma:Inglês
Publicado: 2010
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Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC2836843/
https://ncbi.nlm.nih.gov/pubmed/20085328
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm9015729
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