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131 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28257199 40 Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).EBI Pfizer Inc.
28177228 51 Design, Synthesis, and Biological Evaluation of Coupled Bioactive Scaffolds as Potential Anticancer Agents for Dual Targeting of Dihydrofolate Reductase and Thioredoxin Reductase.EBI National University of Singapore
28258797 32 Synthesis and evaluation of 5-(arylthio)-9H-pyrimido[4,5-b]indole-2,4-diamines as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.EBI Duquesne University
28235702 13 Design, synthesis, biological evaluation and X-ray structural studies of potent human dihydroorotate dehydrogenase inhibitors based on hydroxylated azole scaffolds.EBI University of Torino
6694162 38 Inhibition of human dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(substituted-phenyl)-s-triazine s. A quantitative structure-activity relationship analysis.EBI TBA
27886545 15 Design, synthesis, docking studies and biological evaluation of novel dihydro-1,3,5-triazines as human DHFR inhibitors.EBI Shanghai Institute of Pharmaceutical Industry
27994750 48 Discovery of Potent and Selective Leads againstEBI Turing Pharmaceuticals AG
27437079 30 Charged Nonclassical Antifolates with Activity Against Gram-Positive and Gram-Negative Pathogens.EBI University of Connecticut
26994844 8 Applying the designed multiple ligands approach to inhibit dihydrofolate reductase and thioredoxin reductase for anti-proliferative activity.EBI National University of Singapore
26979156 11 Rational modification of the lead molecule: Enhancement in the anticancer and dihydrofolate reductase inhibitory activity.EBI Guru Nanak Dev University
26617968 4 Design and Synthesis of a Focused Library of Diamino Triazines as Potential Mycobacterium tuberculosis DHFR Inhibitors.EBI Institute of Chemical Technology
25937878 9 The chemistry and pharmacology of privileged pyrroloquinazolines.EBI Oregon Health& Science University
26670841 8 Synthesis, in vitro antitumor activity, dihydrofolate reductase inhibition, DNA intercalation and structure-activity relationship studies of 1,3,5-triazine analogues.EBI Thapar University
25794791 13 Recent advances in the chemistry and biology of pyridopyrimidines.EBI Universit£ d'Orl£ans
25461317 7 Synthetic approaches, functionalization and therapeutic potential of quinazoline and quinazolinone skeletons: the advances continue.EBI University of Nottingham
25127103 4 Structural studies provide clues for analog design of specific inhibitors of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase.EBI Yale University
24913411 13 Elements and modulation of functional dynamics.EBI Janssen Pharmaceutical Research and Development, LLC
24568657 34 Propargyl-linked antifolates are dual inhibitors of Candida albicans and Candida glabrata.EBI University of Connecticut
110934 12 Synthesis and biological activity of 8-oxadihydropteridines.EBI TBA
24428639 56 Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.EBI Trius Therapeutics Inc.
24531230 34 2-[N-Alkyl(R-phenyl)-aminomethyl]-3-phenyl-7-trifluoromethylquinoxalines as anticancer agents inhibitors of folate enzymes.EBI Universit£ degli Studi di Sassari
23665106 5 Synthesis and antiproliferative activity of 4-substituted-piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline.EBI Capital Normal University
23627352 28 Design, synthesis, and molecular modeling of novel pyrido[2,3-d]pyrimidine analogues as antifolates; application of Buchwald-Hartwig aminations of heterocycles.EBI Duquesne University
23375226 22 Structural analysis of the active sites of dihydrofolate reductase from two species of Candida uncovers ligand-induced conformational changes shared among species.EBI University of Connecticut
23273520 93 Ligand-based discovery of N-(1,3-dioxo-1H,3H-benzo[de]isochromen-5-yl)-carboxamide and sulfonamide derivatives as thymidylate synthase A inhibitors.EBI Universit£ degli Studi di Modena e Reggio Emilia
3121854 21 2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 9. Lipophilic trimethoprim analogues as antigonococcal agents.EBI Burroughs Wellcome Co.
7699713 76 Quantitative structure-activity relationships of the inhibition of Pneumocystis carinii dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(X-phenyl)-s-triazines.EBI COR Therapeutics Inc.
7658448 65 Selective inhibitors of Candida albicans dihydrofolate reductase: activity and selectivity of 5-(arylthio)-2,4-diaminoquinazolines.EBI Burroughs Wellcome Company
2502633 23 2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 11. Quinolylmethyl analogues with basic substituents conveying specificity.EBI Wellcome Research Laboratories
3339615 51 Inhibition of murine thymidylate synthase and human dihydrofolate reductase by 5,8-dideaza analogues of folic acid and aminopterin.EBI Medical University of South Carolina
3312605 30 2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 8. The 3,4,5-triethyl isostere of trimethoprim. A study of specificity.EBI Burroughs Wellcome Co.
6772788 8 Folate analogues altered in the C9-N10 bridge region. 16. Synthesis and antifolate activity of 11-thiohomoaminopterin.EBI TBA
7365749 2 Convenient synthesis of 10-deazaaminopterin via a pteridine ylide.EBI TBA
22946585 19 Structure-based selectivity optimization of piperidine-pteridine derivatives as potent Leishmania pteridine reductase inhibitors.EBI Universita` degli Studi di Sassari
23124219 21 Mechanism-based design, synthesis and biological studies of N5-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and potential anticancer agents.EBI Peking University
22739090 86 Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.EBI Duquesne University
22406152 6 Structure aided design of chimeric antibiotics.EBI University of Queensland
19364848 9 Crystal structure of Bacillus anthracis dihydrofolate reductase with the dihydrophthalazine-based trimethoprim derivative RAB1 provides a structural explanation of potency and selectivity.EBI Oklahoma State University
21126002 78 Reducing the brittleness of zein films through chemical modification.EBI Rutgers University
20350811 63 Non-classical antifolates. Part 2: synthesis, biological evaluation, and molecular modeling study of some new 2,6-substituted-quinazolin-4-ones.EBI King Saud University
20092323 23 Single agents with designed combination chemotherapy potential: synthesis and evaluation of substituted pyrimido[4,5-b]indoles as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.EBI Duquesne University
20056546 100 2,4-Diamino-5-methyl-6-substituted arylthio-furo[2,3-d]pyrimidines as novel classical and nonclassical antifolates as potential dual thymidylate synthase and dihydrofolate reductase inhibitors.EBI Duquesne University
19059777 3 Novel non-active site inhibitor of Cryptosporidium hominis TS-DHFR identified by a virtual screen.EBI Yale University
18800768 84 Potent dual thymidylate synthase and dihydrofolate reductase inhibitors: classical and nonclassical 2-amino-4-oxo-5-arylthio-substituted-6-methylthieno[2,3-d]pyrimidine antifolates.EBI Duquesne University
18605720 120 The effect of 5-alkyl modification on the biological activity of pyrrolo[2,3-d]pyrimidine containing classical and nonclassical antifolates as inhibitors of dihydrofolate reductase and as antitumor and/or antiopportunistic infection agents.EBI Duquesne University
17127067 21 Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs.EBI Instituto Superior T£cnico
15615538 28 Synthesis of classical, three-carbon-bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.EBI Duquesne University
15615522 17 Benzoyl ring halogenated classical 2-amino-6-methyl-3,4-dihydro-4-oxo-5-substituted thiobenzoyl-7H-pyrrolo[2,3-d]pyrimidine antifolates as inhibitors of thymidylate synthase and as antitumor agents.EBI Duquesne University
16078850 41 Synthesis of classical, four-carbon bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.EBI Duquesne University
15837298 62 Novel 2-amino-4-oxo-5-arylthio-substituted-pyrrolo[2,3-d]pyrimidines as nonclassical antifolate inhibitors of thymidylate synthase.EBI Duquesne University
12570380 34 Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and as potential antitumor agents.EBI Duquesne University
12408727 38 Synthesis of classical and nonclassical, partially restricted, linear, tricyclic 5-deaza antifolates.EBI Duquesne University
11384244 61 Synthesis, antifolate, and antitumor activities of classical and nonclassical 2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines.EBI Duquesne University
11052790 5 Computational predictions of binding affinities to dihydrofolate reductase: synthesis and biological evaluation of methotrexate analogues.EBI Uppsala University
11052789 49 Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.EBI Duquesne University
10956221 46 Effect of C9-methyl substitution and C8-C9 conformational restriction on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.EBI Duquesne University
9857098 9 Synthesis and potent antifolate activity and cytotoxicity of B-ring deaza analogues of the nonpolyglutamatable dihydrofolate reductase inhibitor Nalpha-(4-amino-4-deoxypteroyl)-Ndelta-hemiphthaloyl- L-ornithine (PT523).EBI Harvard Medical School
8568827 6 Synthesis and biological activity of folic acid and methotrexate analogues containing L-threo-(2S,4S)-4-fluoroglutamic acid and DL-3,3-difluoroglutamic acid.EBI University of Michigan
7877140 74 2,4-Diamino-5-substituted-quinazolines as inhibitors of a human dihydrofolate reductase with a site-directed mutation at position 22 and of the dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.EBI Harvard Medical School
8035423 12 Synthesis and biological activity of N omega-hemiphthaloyl-alpha,omega- diaminoalkanoic acid analogues of aminopterin and 3',5-dichloroaminopterin.EBI Harvard Medical School
1578484 26 Side chain modified 5-deazafolate and 5-deazatetrahydrofolate analogues as mammalian folylpolyglutamate synthetase and glycinamide ribonucleotide formyltransferase inhibitors: synthesis and in vitro biological evaluation.EBI Harvard Medical School
1995880 8 Synthesis and biological activity of methotrexate analogues with two acid groups and a hydrophobic aromatic ring in the side chain.EBI Harvard Medical School
1992122 6 Synthesis and biological activity of the 2-desamino and 2-desamino-2-methyl analogues of aminopterin and methotrexate.EBI Institute
1992118 5 Analogues of methotrexate and aminopterin with gamma-methylene and gamma-cyano substitution of the glutamate side chain: synthesis and in vitro biological activity.EBI Institute
2362285 23 Potent inhibition of thymidylate synthase by two series of nonclassical quinazolines.EBI Warner-Lambert Company
3091832 28 Folate analogues. 26. Syntheses and antifolate activity of 10-substituted derivatives of 5,8-dideazafolic acid and of the poly-gamma-glutamyl metabolites of N10-propargyl-5,8-dideazafolic acid (PDDF).EBI TBA
7069721 2 Molecular structures of 2,4-diaminopyrimidine antifolates with antineoplastic activity.EBI TBA
21788136 26 Synthesis and antimicrobial activity of N¹-benzyl or N¹-benzyloxy-1,6-dihydro-1,3,5-triazine-2,4-diamines.EBI Huazhong University of Science and Technology
21831637 52 Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.EBI Trius Therapeutics, San Diego, CA 92121, United States.
21550809 44 Design, synthesis, biological evaluation and X-ray crystal structure of novel classical 6,5,6-tricyclic benzo[4,5]thieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors.EBI Duquesne University
20606069 18 Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1.EBI Oklahoma State University
20350951 4 Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.EBI Kenya Medical Research Institute/Wellcome Trust Collaborative Research Program
20527892 7 Novel approaches for targeting thymidylate synthase to overcome the resistance and toxicity of anticancer drugs.EBI Institute of Theoretical Studies gGmbH
20452776 29 Synthesis and characterization of potent inhibitors of Trypanosoma cruzi dihydrofolate reductase.EBI University of Alabama
20166671 85 Selectively nonselective kinase inhibition: striking the right balance.EBI Schering-Plough
19560363 118 In vitro biological activity and structural analysis of 2,4-diamino-5-(2'-arylpropargyl)pyrimidine inhibitors of Candida albicans.EBI University of Connecticut
17875993 24 In vitro efficacy of new antifolates against trimethoprim-resistant Bacillus anthracis.EBI Oklahoma State University
 4 Synthesis and biological evaluation of a new series of dihydrofolate reductase inhibitors based on the 4-(2,6-diamino-5-pyrimidinyl)alkyl-L-glutamic acid structureEBI TBA
18555562 6 Novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives as dihydrofolate inhibitor: design, synthesis and antifolate activity.EBI Peking University
17532099 30 Synthesis of N-(5,7-diamino-3-phenyl-quinoxalin-2-yl)-3,4,5-substituted anilines and N-[4[(5,7-diamino-3-phenylquinoxalin-2-yl)amino]benzoyl]-l-glutamic acid diethyl ester: evaluation of in vitro anti-cancer and anti-folate activities.EBI Università degli Studi di Sassari
18205293 14 Synthesis and biological evaluation of novel 2,4-diaminoquinazoline derivatives as SMN2 promoter activators for the potential treatment of spinal muscular atrophy.EBI deCODE Chemistry Inc
17569517 7 Novel boron-containing, nonclassical antifolates: synthesis and preliminary biological and structural evaluation.EBI Southern Research Institute
15615544 6 Synthesis and in vitro antifolate activity of rotationally restricted aminopterin and methotrexate analogues.EBI Harvard Medical School
15115391 56 Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase.EBI Harvard Medical School
14998335 69 New 2,4-diamino-5-(2',5'-substituted benzyl)pyrimidines as potential drugs against opportunistic infections of AIDS and other immune disorders. Synthesis and species-dependent antifolate activity.EBI Harvard Medical School
12773035 56 Novel dihydrofolate reductase inhibitors. Structure-based versus diversity-based library design and high-throughput synthesis and screening.EBI F. Hoffmann-La Roche Ltd.
11960504 14 Synthesis of N-[4-[1-ethyl-2-(2,4-diaminofuro[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid as an antifolate.EBI Duquesne University
11931624 6 Synthesis and in vitro antitumor activity of new deaza analogues of the nonpolyglutamatable antifolate N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine (PT523).EBI Harvard Medical School
11881993 175 Development of 2,4-diaminopyrimidines as antimalarials based on inhibition of the S108N and C59R+S108N mutants of dihydrofolate reductase from pyrimethamine-resistant Plasmodium falciparum.EBI National Center for Genetic Engineering and Biotechnology
11754578 155 Pharmacophore mapping of a series of 2,4-diamino-5-deazapteridine inhibitors of Mycobacterium avium complex dihydrofolate reductase.EBI Lindsley F. Kimball Research Institute
10543874 79 Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase.EBI Cardiff University
10360757 14 The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase.EBI Cardiff University
9990460 9 The synthesis and biological activity of a series of 2,4-diaminopyrido[2,3-d]pyrimidine based antifolates as antineoplastic and antiarthritic agents.EBI Lilly Research Laboratories
9719595 120 Structure-based design and synthesis of lipophilic 2,4-diamino-6-substituted quinazolines and their evaluation as inhibitors of dihydrofolate reductases and potential antitumor agents.EBI Duquesne University
8691474 111 2,4-diamino-5-deaza-6-substituted pyrido[2,3-d]pyrimidine antifolates as potent and selective nonclassical inhibitors of dihydrofolate reductases.EBI Duquesne University
8691451 7 Synthesis and biological evaluation of N alpha-(4-amino-4-deoxy-10-methylpteroyl)-DL-4,4-difluoroornithine.EBI University of Michigan
8632413 38 High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size.EBI Wellcome Research Laboratories
8568828 2 Synthesis and biological evaluation of DL-4,4-difluoroglutamic acid and DL-gamma,gamma-difluoromethotrexate.EBI University of Michigan
8230134 48 Synthesis of 5-methyl-5-deaza nonclassical antifolates as inhibitors of dihydrofolate reductases and as potential antipneumocystis, antitoxoplasma, and antitumor agents.EBI Duquesne University
8230096 79 2,4-Diaminothieno[2,3-d]pyrimidine analogues of trimetrexate and piritrexim as potential inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.EBI Harvard Medical School
8164259 44 Classical and nonclassical furo[2,3-d]pyrimidines as novel antifolates: synthesis and biological activities.EBI Duquesne University
7990119 91 Structure-activity relationships and pH dependence of binding of 8-alkyl-N5-deazapterins to dihydrofolate reductase.EBI University of Sydney
7562910 18 Effect of bridge region variation on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.EBI Duquesne University
7473577 11 5-Arylthio-substituted 2-amino-4-oxo-6-methylpyrrolo[2,3-d]pyrimidine antifolates as thymidylate synthase inhibitors and antitumor agents.EBI Duquesne University
6403710 6 Folate analogues. 21. Synthesis and antifolate and antitumor activities of N10-(cyanomethyl)-5,8-dideazafolic acid.EBI TBA
2918496 3 The 2-desamino and 2-desamino-2-methyl analogues of aminopterin do not inhibit dihydrofolate reductase but are potently toxic to tumor cells in culture.EBI Harvard Medical School
2754716 18 2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 13. Some alkenyl derivatives with high in vitro activity against anaerobic organisms.EBI Wellcome Research Laboratories
2542557 14 Folate analogues. 32. Synthesis and biological evaluation of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid and related compounds.EBI University of South Alabama
2296020 18 Synthesis and antifolate properties of 9-alkyl-10-deazaminopterins.EBI SRI International
2016722 8 Synthesis and in vitro biological activity of new deaza analogues of folic acid, aminopterin, and methotrexate with an L-ornithine side chain.EBI Harvard Medical School
1992121 13 Folate analogues. 34. Synthesis and antitumor activity of non-polyglutamylatable inhibitors of dihydrofolate reductase.EBI University of South Alabama
1433179 13 5,10-Methylenetetrahydro-5-deazafolic acid and analogues: synthesis and biological activities.EBI Duquesne University
22957721 3 In vitro effects of cinnamic acid derivatives on protein tyrosine phosphatase 1B.BDB Chulalongkorn University
22630073 12 Susceptibility of cord blood antioxidant enzymes glutathione reductase, glutathione peroxidase and glutathione S-transferase to different antibiotics: in vitro approach.BDB Ondokuz Mayis University
16469866 21 Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist.BDB ACADIA Pharmaceuticals Inc.
11082453 77 ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.BDB Abbott Laboratories
9247853 7 Yeast hexokinase inhibitors designed from the 3-D enzyme structure rebuilding.BDB Groupe de Chimie Organique Biologique
6655559 46 Comparison of dopamine receptor sites labeled by [3H]-S-sulpiride and [3H]-spiperone in striatum.BDB University of California
2385234 35 Binding of selective antagonists to four muscarinic receptors (M1 to M4) in rat forebrain.BDB Université Libre de Bruxelles