The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 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). |
Pfizer |
| 28177228 |
51 |
Design, Synthesis, and Biological Evaluation of Coupled Bioactive Scaffolds as Potential Anticancer Agents for Dual Targeting of Dihydrofolate Reductase and Thioredoxin Reductase. |
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. |
Duquesne University |
| 28235702 |
13 |
Design, synthesis, biological evaluation and X-ray structural studies of potent human dihydroorotate dehydrogenase inhibitors based on hydroxylated azole scaffolds. |
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. |
TBA |
| 27886545 |
15 |
Design, synthesis, docking studies and biological evaluation of novel dihydro-1,3,5-triazines as human DHFR inhibitors. |
Shanghai Institute of Pharmaceutical Industry |
| 27994750 |
48 |
Discovery of Potent and Selective Leads against |
Turing Pharmaceuticals |
| 27437079 |
30 |
Charged Nonclassical Antifolates with Activity Against Gram-Positive and Gram-Negative Pathogens. |
University of Connecticut |
| 26994844 |
8 |
Applying the designed multiple ligands approach to inhibit dihydrofolate reductase and thioredoxin reductase for anti-proliferative activity. |
National University of Singapore |
| 26979156 |
11 |
Rational modification of the lead molecule: Enhancement in the anticancer and dihydrofolate reductase inhibitory activity. |
Guru Nanak Dev University |
| 26617968 |
4 |
Design and Synthesis of a Focused Library of Diamino Triazines as Potential Mycobacterium tuberculosis DHFR Inhibitors. |
Institute of Chemical Technology |
| 25937878 |
9 |
The chemistry and pharmacology of privileged pyrroloquinazolines. |
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. |
Thapar University |
| 25794791 |
13 |
Recent advances in the chemistry and biology of pyridopyrimidines. |
Universit£ |
| 25461317 |
7 |
Synthetic approaches, functionalization and therapeutic potential of quinazoline and quinazolinone skeletons: the advances continue. |
University of Nottingham |
| 25127103 |
4 |
Structural studies provide clues for analog design of specific inhibitors of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase. |
Yale University |
| 24913411 |
13 |
Elements and modulation of functional dynamics. |
Janssen Research and Development |
| 24568657 |
34 |
Propargyl-linked antifolates are dual inhibitors of Candida albicans and Candida glabrata. |
University of Connecticut |
| 110934 |
12 |
Synthesis and biological activity of 8-oxadihydropteridines. |
TBA |
| 24428639 |
56 |
Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines. |
Trius Therapeutics |
| 24531230 |
34 |
2-[N-Alkyl(R-phenyl)-aminomethyl]-3-phenyl-7-trifluoromethylquinoxalines as anticancer agents inhibitors of folate enzymes. |
Universit£ |
| 23665106 |
5 |
Synthesis and antiproliferative activity of 4-substituted-piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline. |
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. |
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. |
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. |
Universit£ |
| 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. |
Cor Therapeutics |
| 6772788 |
8 |
Folate analogues altered in the C9-N10 bridge region. 16. Synthesis and antifolate activity of 11-thiohomoaminopterin. |
TBA |
| 22946585 |
19 |
Structure-based selectivity optimization of piperidine-pteridine derivatives as potent Leishmania pteridine reductase inhibitors. |
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. |
Peking University |
| 22739090 |
86 |
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents. |
Duquesne University |
| 22406152 |
6 |
Structure aided design of chimeric antibiotics. |
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. |
Oklahoma State University |
| 21126002 |
39 |
Reducing the brittleness of zein films through chemical modification. |
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. |
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. |
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. |
Duquesne University |
| 19059777 |
3 |
Novel non-active site inhibitor of Cryptosporidium hominis TS-DHFR identified by a virtual screen. |
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. |
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. |
Duquesne University |
| 17127067 |
21 |
Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs. |
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. |
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. |
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. |
Duquesne University |
| 15837298 |
62 |
Novel 2-amino-4-oxo-5-arylthio-substituted-pyrrolo[2,3-d]pyrimidines as nonclassical antifolate inhibitors of thymidylate synthase. |
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. |
Duquesne University |
| 12408727 |
38 |
Synthesis of classical and nonclassical, partially restricted, linear, tricyclic 5-deaza antifolates. |
Duquesne University |
| 11384244 |
61 |
Synthesis, antifolate, and antitumor activities of classical and nonclassical 2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines. |
Duquesne University |
| 11052790 |
5 |
Computational predictions of binding affinities to dihydrofolate reductase: synthesis and biological evaluation of methotrexate analogues. |
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. |
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. |
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). |
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. |
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. |
Harvard Medical School |
| 8035423 |
12 |
Synthesis and biological activity of N omega-hemiphthaloyl-alpha,omega- diaminoalkanoic acid analogues of aminopterin and 3',5-dichloroaminopterin. |
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. |
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. |
Harvard Medical School |
| 1992122 |
6 |
Synthesis and biological activity of the 2-desamino and 2-desamino-2-methyl analogues of aminopterin and methotrexate. |
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. |
Institute |
| 2362285 |
23 |
Potent inhibition of thymidylate synthase by two series of nonclassical quinazolines. |
Warner-Lambert |
| 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). |
TBA |
| 7069721 |
2 |
Molecular structures of 2,4-diaminopyrimidine antifolates with antineoplastic activity. |
TBA |
| 21788136 |
26 |
Synthesis and antimicrobial activity of N¹-benzyl or N¹-benzyloxy-1,6-dihydro-1,3,5-triazine-2,4-diamines. |
Huazhong University of Science and Technology |
| 21831637 |
52 |
Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines. |
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. |
Duquesne University |
| 20606069 |
18 |
Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1. |
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. |
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. |
Institute of Theoretical Studies Ggmbh |
| 20452776 |
29 |
Synthesis and characterization of potent inhibitors of Trypanosoma cruzi dihydrofolate reductase. |
University of Alabama |
| 20166671 |
85 |
Selectively nonselective kinase inhibition: striking the right balance. |
Schering-Plough |
| 19560363 |
118 |
In vitro biological activity and structural analysis of 2,4-diamino-5-(2'-arylpropargyl)pyrimidine inhibitors of Candida albicans. |
University of Connecticut |
| 17875993 |
24 |
In vitro efficacy of new antifolates against trimethoprim-resistant Bacillus anthracis. |
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 structure |
TBA |
| 18555562 |
6 |
Novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives as dihydrofolate inhibitor: design, synthesis and antifolate activity. |
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. |
Università |
| 18205293 |
14 |
Synthesis and biological evaluation of novel 2,4-diaminoquinazoline derivatives as SMN2 promoter activators for the potential treatment of spinal muscular atrophy. |
Decode Chemistry |
| 17569517 |
7 |
Novel boron-containing, nonclassical antifolates: synthesis and preliminary biological and structural evaluation. |
Southern Research Institute |
| 15615544 |
6 |
Synthesis and in vitro antifolate activity of rotationally restricted aminopterin and methotrexate analogues. |
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. |
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. |
Harvard Medical School |
| 12773035 |
56 |
Novel dihydrofolate reductase inhibitors. Structure-based versus diversity-based library design and high-throughput synthesis and screening. |
F. Hoffmann-La Roche |
| 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. |
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). |
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. |
National Center For Genetic Engineering and Biotechnology At Thailand |
| 11754578 |
155 |
Pharmacophore mapping of a series of 2,4-diamino-5-deazapteridine inhibitors of Mycobacterium avium complex dihydrofolate reductase. |
Lindsley F. Kimball Research Institute |
| 10543874 |
79 |
Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase. |
Cardiff University |
| 10360757 |
14 |
The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase. |
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. |
Eli Lilly |
| 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. |
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. |
Duquesne University |
| 8691451 |
7 |
Synthesis and biological evaluation of N alpha-(4-amino-4-deoxy-10-methylpteroyl)-DL-4,4-difluoroornithine. |
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. |
Wellcome Research Laboratories |
| 8568828 |
2 |
Synthesis and biological evaluation of DL-4,4-difluoroglutamic acid and DL-gamma,gamma-difluoromethotrexate. |
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. |
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. |
Harvard Medical School |
| 8164259 |
44 |
Classical and nonclassical furo[2,3-d]pyrimidines as novel antifolates: synthesis and biological activities. |
Duquesne University |
| 7990119 |
91 |
Structure-activity relationships and pH dependence of binding of 8-alkyl-N5-deazapterins to dihydrofolate reductase. |
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. |
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. |
Duquesne University |
| 6403710 |
6 |
Folate analogues. 21. Synthesis and antifolate and antitumor activities of N10-(cyanomethyl)-5,8-dideazafolic acid. |
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. |
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. |
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. |
University of South Alabama |
| 2296020 |
18 |
Synthesis and antifolate properties of 9-alkyl-10-deazaminopterins. |
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. |
Harvard Medical School |
| 1992121 |
13 |
Folate analogues. 34. Synthesis and antitumor activity of non-polyglutamylatable inhibitors of dihydrofolate reductase. |
University of South Alabama |
| 1433179 |
13 |
5,10-Methylenetetrahydro-5-deazafolic acid and analogues: synthesis and biological activities. |
Duquesne University |
| 22957721 |
3 |
In vitro effects of cinnamic acid derivatives on protein tyrosine phosphatase 1B. |
Chulalongkorn University |
| 22630073 |
12 |
Susceptibility of cord blood antioxidant enzymes glutathione reductase, glutathione peroxidase and glutathione S-transferase to different antibiotics: in vitro approach. |
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. |
Acadia Pharmaceuticals |
| 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. |
Abbott Laboratories |
| 9247853 |
7 |
Yeast hexokinase inhibitors designed from the 3-D enzyme structure rebuilding. |
Universite Paul Sabatier |
| 6655559 |
46 |
Comparison of dopamine receptor sites labeled by [3H]-S-sulpiride and [3H]-spiperone in striatum. |
University of California |
| 2385234 |
35 |
Binding of selective antagonists to four muscarinic receptors (M1 to M4) in rat forebrain. |
UniversitÉ |
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