Discovery of 6-substituted thieno[2,3-d]pyrimidine analogs as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis in folate receptor expressing human tumors

We discovered 6-substituted thieno[2,3-d]pyrimidine compounds (3–9) with 3–4 bridge carbons and side-chain thiophene or furan rings for dual targeting one-carbon (C1) metabolism in folate receptor- (FR) expressing cancers. Synthesis involved nine steps starting from the bromo-aryl carboxylate. From...

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Publicado no:Bioorg Med Chem
Main Authors: Wallace-Povirk, Adrianne, Tong, Nian, Wong-Roushar, Jennifer, O’Connor, Carrie, Zhou, Xilin, Hou, Zhanjun, Bao, Xun, Garcia, Gloria E., Li, Jing, Kim, Seongho, Dann, Charles E., Matherly, Larry H., Gangjee, Aleem
Formato: Artigo
Idioma:Inglês
Publicado em: 2021
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC8058616/
https://ncbi.nlm.nih.gov/pubmed/33773393
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmc.2021.116093
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