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.

doi:10.1016/j.bmc.2021.116093

Paper

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.

Published Feb 26, 2021 · Adrianne Wallace-Povirk, Nian Tong, Jennifer Wong-Roushar

Bioorganic & medicinal chemistry

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8

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Abstract

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In Vitro Study

Study Snapshot

6-substituted thieno[2,3-d]pyrimidine analogs show potential as selective multi-targeted anti-tumor agents by targeting one-carbon metabolism and de novo purine biosynthesis in folate receptor-expressing cancers.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

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.

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References

Therapeutic Targeting of Mitochondrial One-Carbon Metabolism in Cancer

Targeting mitochondrial one-carbon metabolism in cancer cells offers potential therapeutic benefits, as it plays a crucial role in metabolic homeostasis and its relationship with the oncogenic phenotype.

Design, synthesis and biological evaluation of novel pyrrolo[2,3-d]pyrimidine as tumor-targeting agents with selectivity for tumor uptake by high affinity folate receptors over the reduced folate carrier.

Novel pyrrolo[2,3-d]pyrimidine compounds show increased tumor cell inhibition and selectivity for high affinity folate receptors over the reduced folate carrier, offering potential advantages over current antifolates.

Multitarget Anticancer Agents Based on Histone Deacetylase and Protein Kinase CK2 Inhibitors

Multitargeting HDAC and CK2 inhibitors show potential as a novel cancer treatment, with N-Hydroxy-8-(4,5,6,7-tetrabromo-2-(dimethylamino)-1H-benzo[d]imidazol-1-yl)o

One-Carbon Metabolism Supports S-Adenosylmethionine and Histone Methylation to Drive Inflammatory Macrophages.

One-carbon metabolism synergistically drives inflammation in macrophages by fueling the generation of S-adenosylmethionine (SAM), which is essential for IL-1 production and chromatin state.

New approaches to cancer therapy: combining Fatty Acid Amide Hydrolase (FAAH) inhibition with Peroxisome Proliferator-Activated Receptors (PPARs) activation.

Novel FAAH inhibitors that act as PPAR agonists show promising potential as leads for the discovery of highly effective anti-cancer compounds.

Citations

From pollen to putrid: Comparative metagenomics reveals how microbiomes support dietary specialization in vulture bees

Vulture bees' microbiomes have evolved to adapt to consuming carrion, potentially protecting them from opportunistic pathogens and cellular stress.

Design and one-pot synthesis of new substituted pyrrolo[1,2-a]thieno[3,2-e]pyrimidine as potential antitumor agents: in vitro and in vivo studies.

The lead compound 12aa shows high potential in treating melanoma by inducing cell apoptosis and requiring low-cost starting chemicals for synthesis.

Discovery of Tumor-Targeted 6-Methyl Substituted Pemetrexed and Related Antifolates with Selective Loss of RFC Transport

Adding a 6-methyl moiety to 5-substituted pyrrolo[2,3-d]pyrimidine antifolates allows for selective tumor transport while preserving antitumor efficacy.

Structure-Based Design of Transport-Specific Multitargeted One-Carbon Metabolism Inhibitors in Cytosol and Mitochondria

Multitargeted agents offer improved tumor selectivity and potency in targeted cancer therapy, offering advantages over clinically used antifolates.

Multitargeted 6-Substituted Thieno[2,3-d]pyrimidines as Folate Receptor-Selective Anticancer Agents that Inhibit Cytosolic and Mitochondrial One-Carbon Metabolism

6-substituted thieno[2,3-d]pyrimidines show potential as potent multitargeted antitumor agents with folate receptor transport selectivity and inhibition of cytosolic and mitochondrial one-carbon metabolism.