"GARFTase" · 9 results · Global ETD Search

Synthesis of novel 5-substituted pyrrolo[2,3-d]pyrimidine antifolates as selective and potent anti-tumor agents

Karim, Mohammad2019

… and/or PCFT and over RFC targets inhibition of GARFTase dependent salvage pathway for purine biosynthesis inside the tumor. Based on this premise, five 5-substituted pyrrolo[2,3-d]pyrimidines have been designed, synthesized and characterized. Among them four are novel compounds and one …

duquesne Repository record for Synthesis of novel 5-substituted pyrrolo[2,3-d]pyrimidine antifolates as selective and potent anti-tumor agents (opens in a new tab)

Discovery of Pyrimidine-based Heterocycles as Single Agents With Combination Chemotherapy Potential And As Inhibitors Of Purine Nucleotide Biosynthesis For The Treatment of Cancer

Mohan, Rishabh2018

… bridge substitution as GARFTase inhibitors. The work in this dissertation is centered on identifying structural features that are necessary for inhibition of tubulin polymerization as well as for inhibition of one or more of the receptor tyrosine …

duquesne Repository record for Discovery of Pyrimidine-based Heterocycles as Single Agents With Combination Chemotherapy Potential And As Inhibitors Of Purine Nucleotide Biosynthesis For The Treatment of Cancer (opens in a new tab)

Classical Antifolates: Synthesis of 5-Substituted, 6-Substituted and 7-Substituted Pyrrolo[2,3-d]Pyrimidines as Targeted Anticancer Therapies

Wang, Yiqiang2018

… or/and PCFT and tumor targeted antifolates with GARFTase or multiple folate metabolizing enzyme inhibition. The design strategies employed include: variation of the side chain substitution position (5-, 6- and 7-substituted); variation of the side chain length (n=1-6); isosteric …

duquesne Repository record for Classical Antifolates: Synthesis of 5-Substituted, 6-Substituted and 7-Substituted Pyrrolo[2,3-d]Pyrimidines as Targeted Anticancer Therapies (opens in a new tab)

Synthesis of Bicyclic Thieno[2,3-d]Pyrimidines, Tricyclic Thieno[2,3-d]Pyrimidines and Thieno[3,2-d]Pyrimidines as Classical and Nonclassical Antifolates

Zhou, Xilin2018

… glycinamide ribonucleotide formyltransferase (GARFTase) are important folate dependent enzymes that are targets for cancer chemotherapy and the treatment of infectious diseases. As a part of this study, thirty-five novel compounds were designed and synthesized on the basis of existing …

duquesne Repository record for Synthesis of Bicyclic Thieno[2,3-d]Pyrimidines, Tricyclic Thieno[2,3-d]Pyrimidines and Thieno[3,2-d]Pyrimidines as Classical and Nonclassical Antifolates (opens in a new tab)

Synthesis of furo[2,3-d]pyrimidines, thieno[2,3- d]pyrimidines, pyrrolo[2,3-d]pyrimidines as classical and nonclassical antifolates, receptor tyrosine kinase (RTK) inhibitors and antimitotic agents

Zhang, Xin2018

… glycinamide ribonucleotide formyltransferase (GARFTase) are important folate dependent enzymes that are targets for cancer chemotherapy and the treatment of infectious diseases. Classical antifolates, in most cases, are substrates for folypoly - γ - glutamate synthase (FPGS) and rely on folate …

duquesne Repository record for Synthesis of furo[2,3-d]pyrimidines, thieno[2,3- d]pyrimidines, pyrrolo[2,3-d]pyrimidines as classical and nonclassical antifolates, receptor tyrosine kinase (RTK) inhibitors and antimitotic agents (opens in a new tab)

Design and Synthesis of Pyrimidine Based Heterocycles as Potential Anti-cancer Agents with Combination Chemotherapeutic Potential or Targeted One Carbon Metabolism Inhibition and Anti-opportunistic Agents

Doshi, Arpit2020

… as targeted one-carbon metabolism enzymes (GARFTase/AICARFTase and/or SHMT2) inhibitors circumventing both dose-limiting toxicity and tumor resistance associated with most prescribed antitumor agents like pemetrexed. PCP is a host species-specific infection. Current therapies such as …

duquesne Repository record for Design and Synthesis of Pyrimidine Based Heterocycles as Potential Anti-cancer Agents with Combination Chemotherapeutic Potential or Targeted One Carbon Metabolism Inhibition and Anti-opportunistic Agents (opens in a new tab)

The proton-coupled folate transporter: biology and therapeutic applications to cancer

Desmoulin, Sita2012

… ribonucleotide (GAR) formyltransferase (GARFTase) in the de novo purine biosynthesis pathway as the principle drug target. This was confirmed by in situ measurement of [14C]glycine incorporation into [14C]formylGAR in treated cells. Furthermore, contraction of intracellular purine …

wayne-thes Repository record for The proton-coupled folate transporter: biology and therapeutic applications to cancer (opens in a new tab)

Pyrrolo[2,3-d]pyrimidine Classical Antifolates for Targeted Cancer Chemotherapy- Applications of Bioisosteric and Regioisomeric Substitutions for Improved Tumor-Selectivity and Potency

Punaha Ravindra, Manasa2019

… pemetrexed (PMX; TS and GARFTase inhibitor), pralatrexate (PTX; DHFR inhibitor), and raltitrexed (RTX; TS inhibitor), have two major disadvantages: (1) dose-limiting toxicities due to ubiquitous transport via the reduced folate carrier …

duquesne Repository record for Pyrrolo[2,3-d]pyrimidine Classical Antifolates for Targeted Cancer Chemotherapy- Applications of Bioisosteric and Regioisomeric Substitutions for Improved Tumor-Selectivity and Potency (opens in a new tab)

Synthesis of 2,4,6-Substituted Pyrrolo[2,3-d]pyrimidines as Potential Anticancer Agents

Yang, Si2018

This thesis mainly focuses on the introduction of the background and work have been done in the areas of antifolates development, such as folate function, its three uptake mechanisms inside human cells, antifolates’ role in chemotherapy, et. al. In addition, the …

duquesne Repository record for Synthesis of 2,4,6-Substituted Pyrrolo[2,3-d]pyrimidines as Potential Anticancer Agents (opens in a new tab)

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