Synthesis, biological and antitumor activity of a highly potent 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitor with proton-coupled folate transporter and folate receptor selectivity over the reduced folate carrier that inhibits β-glycinamide ribonucleotide formyltransferase

2-Amino-4-oxo-6-substituted pyrrolo[2,3-d]pyrimidine antifolates with a thienoyl side chain (compounds 1–3, respectively) were synthesized for comparison with compound 4, the previous lead compound of this series. Conversion of hydroxyl acetylen-thiophene carboxylic esters to thiophenyl-α-bromomethy...

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Main Authors: Wang, Lei, Desmoulin, Sita Kugel, Cherian, Christina, Polin, Lisa, White, Kathryn, Kushner, Juiwanna, Fulterer, Andreas, Chang, Min-Hwang, Mitchell, Shermaine, Stout, Mark, Romero, Michael F., Hou, Zhanjun, Matherly, Larry H., Gangjee, Aleem
Formato: Artigo
Idioma:Inglês
Publicado: 2011
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC3209708/
https://ncbi.nlm.nih.gov/pubmed/21879757
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm200739e
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