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Showing 1 to 17 of 17 for “"Antifolates"”.
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Investigation of the effects of antifolates on Escherichia coli 1810.
The Gel electrophoresis procedure was employed in the investigation of the effect of Trimethoprim (TMP), Sulphadiazine (SD) and p-Aminobenzoic acid (pABA) on the outer membrane and peptidoglycan (OM-PG) associated proteins in the test bacteria. The test organisms were the sensitive Escherichia coli …
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Synthesis of 2,4,6-Substituted Pyrrolo[2,3-d]pyrimidines as Potential Anticancer Agents
… 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, <em>et. al</em>. In addition, the Structure-Activity-Relationship design rationale for the series of antifolates …
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Synthesis of Novel 6-Substituted and 5-Substituted Pyrrolo[2,3-D] Pyrimidine Antifolates as Targeted Anticancer Therapies
… and current research progress in the areas of antifolates and chemotherapy of anticancer. The design and synthesis of classical 6- substituted pyrrolo[2,3-<em>d</em>]pyrimidines and 5-substituted pyrrolo[2,3-<em>d</em>]pyrimidines as potential antifolates have been described. The design …
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Synthesis of novel 5-substituted pyrrolo[2,3-d]pyrimidine antifolates as selective and potent anti-tumor agents
… (RTX): are a few examples of classical antifolates that are currently in clinical use. Although these compounds are widely used, all of them show dose limiting toxicity due to their non-specific transport into normal cells as well as malignant cells. Currently, clinically used classical …
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The proton-coupled folate transporter: biology and therapeutic applications to cancer
… pathways has been achieved through the use of antifolates. Unfortunately, the efficacy of many clinically approved antifolates is limited by a lack of tumor selectivity. Facilitative transport of folates into mammalian cells is achieved by the reduced folate carrier (RFC) and proton-coupled …
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Folate transport and drug resistance in the African Trypanosome
… of these substrates was inhibited by classical antifolates, but not by non-classical antifolates. Genome-wide RNAi library screens with methotrexate and raltitrexed identified the putative folate transporter genes to be involved in drug resistance. RNAi knockdown of the folate transport genes …
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Classical Antifolates: Synthesis of 5-Substituted, 6-Substituted and 7-Substituted Pyrrolo[2,3-d]Pyrimidines as Targeted Anticancer Therapies
… research progress in the area of classical antifolates as the targeted anticancer therapies.</p><p> In this study, twelve series of classical 5-, 6- and 7-substituted pyrrolo[2, 3-d]pyrimidines were designed and synthesized. Extensive structure modifications of the pyrrolo[2, 3-d] pyrimidine …
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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
… background and research progress in the areas of antifolates and antimitotic agents has been reviewed and discussed. Thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFTase) are important folate dependent enzymes that are targets for …
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Pyrrolo[2,3-d]pyrimidine Classical Antifolates for Targeted Cancer Chemotherapy- Applications of Bioisosteric and Regioisomeric Substitutions for Improved Tumor-Selectivity and Potency
… of resistance.</p> <p>Clinically used antifolates methotrexate (<strong>MTX</strong>; DHFR inhibitor), pemetrexed (<strong>PMX</strong>; TS and GARFTase inhibitor), pralatrexate (<strong>PTX</strong>; DHFR inhibitor), and raltitrexed (<strong>RTX</strong>; TS inhibitor), have two major …
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The Therapeutic Targeting Of Folate Receptor Alpha Positive Tumors Via Folate Receptor Selective Novel 5- And 6- Substituted Pyrrolo [2,3-D]pyrimidine Antifolates"
… most treatments fail. The clinically approved antifolates, MTX and PMX, have greatly improved treatment outcomes in a number of malignancies, however they have been implicated in dose-limiting toxicities that are thought to arise from uptake mediated by the ubiquitously express protein, the …
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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
… background and research progress in the areas of antifolates, receptor tyrosine kinase (RTK) inhbitors and anti mitotic agents has been discussed. Thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFTase) are important folate dependent …
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Single Nucleotide Polymorphisms in the Folypoly-gamma-glutamate synthetase Gene
… Similarly, in the case of cancer chemotherapy, antifolates, such as Lometrexol and Tomudex are retained in cells through the activity of FPGS. Consequently, any single nucleotide polymorphisms (SNPs) that exist in the fpgs gene may decrease or increase the cytotoxicity of antifolates and, …
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Design and synthesis of potential antimicrobial agents
… DHFR provided opportunity to design new antifolates. The new antifolates described herein were designed to retain the pharmcophore of pyrimethamine (2,4- diamino-5(4-chlorophenyl)-6-ethylpyrimidine), but encompassing a range of polar groups that might interact with the M. tuberculosis …
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Synthesis of pyrrolo[2,3-d]pyrimidines and pyrazino[2,3-d]pyrimidines and their biological activities
… activities to eventually produce potential new antifolates. Funtionalised nitroalkenes were successfully added to the C5 of 2-thioalkyl-6-amino-4-oxopyrimidines via a Michael reaction. Subsequent cyclisation was accomplished by a Nef reaction using a titanium(III) chloride mediated system. …
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Antibiotic Drug Discovery Targeting Bacterial Metabolism
… guides the development of next-generation antifolates designed to avoid these characterized resistance strategies. In the subsequent chapter, a conditional metabolic screening approach was employed to discover inhibitors disrupting metabolic pathways related to folate biosynthesis. The …
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The mechanistic basis of susceptibility and resistance to the antitubercular drug para-aminosalicylic acid
… acid (PABA), is a known antagonist of antifolates, namely sulfonamides. Since PAS was shown to act similarly to PABA in folate biosynthesis, PAS-sulfonamide interactions were tested against a panel of bacterial pathogens. PAS could antagonize sulfonamides in all of these organisms. …