The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 25427005 |
42 |
Alanine mutants of the interface residues of human thymidylate synthase decode key features of the binding mode of allosteric anticancer peptides. |
University of California San Francisco |
| 25127103 |
4 |
Structural studies provide clues for analog design of specific inhibitors of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase. |
Yale University |
| 430474 |
2 |
trans-5-(3,3,3-Trifluoro-1-propenyl-)-2'-deoxyuridylate: a mechanism-based inhibitor of thymidylate synthetase. |
TBA |
| 24531230 |
34 |
2-[N-Alkyl(R-phenyl)-aminomethyl]-3-phenyl-7-trifluoromethylquinoxalines as anticancer agents inhibitors of folate enzymes. |
Universit£ |
| 24470841 |
9 |
Discovery of potent and selective inhibitors of |
Duquesne University |
| 24147825 |
22 |
2'-Deoxyuridine 5'-monophosphate substrate displacement in thymidylate synthase through 6-hydroxy-2H-naphtho[1,8-bc]furan-2-one derivatives. |
University of Modena and Reggio Emilia |
| 24125851 |
48 |
Novel acetamidothiazole derivatives: synthesis and in vitro anticancer evaluation. |
University of Mansoura |
| 23665106 |
5 |
Synthesis and antiproliferative activity of 4-substituted-piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline. |
Capital Normal University |
| 23490159 |
13 |
Novel 1,3,4-oxadiazole thioether derivatives targeting thymidylate synthase as dual anticancer/antimicrobial agents. |
Nanjing University |
| 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£ |
| 20153089 |
97 |
3D-QSAR studies on quinazoline antifolate thymidylate synthase inhibitors by CoMFA and CoMSIA models. |
Meerut Institute of Engineering and Technology |
| 2909728 |
5 |
Quinazoline antifolates inhibiting thymidylate synthase: synthesis of four oligo(L-gamma-glutamyl) conjugates of N10-propargyl-5,8-dideazafolic acid and their enzyme inhibition. |
Pedagogical University |
| 23075414 |
7 |
Inhibitor of ovarian cancer cells growth by virtual screening: a new thiazole derivative targeting human thymidylate synthase. |
Universit£ |
| 22946585 |
19 |
Structure-based selectivity optimization of piperidine-pteridine derivatives as potent Leishmania pteridine reductase inhibitors. |
Universita` Degli Studi Di Sassari |
| 22739090 |
86 |
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents. |
Duquesne 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 |
| 18362071 |
3 |
A molecular modeling study of the interaction of 2'-fluoro-substituted analogues of dUMP/FdUMP with thymidylate synthase. |
Polish Academy of Sciences |
| 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 |
| 15214773 |
76 |
Fragment-based drug discovery. |
Sunesis Pharmaceuticals |
| 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 |
| 11384244 |
61 |
Synthesis, antifolate, and antitumor activities of classical and nonclassical 2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines. |
Duquesne 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 |
| 8917645 |
20 |
Synthesis and biological activity of aromatic amino acid phosphoramidates of 5-fluoro-2'-deoxyuridine and 1-beta-arabinofuranosylcytosine: evidence of phosphoramidase activity. |
University of Minnesota |
| 8917644 |
49 |
2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines as nonclassical antifolate inhibitors of thymidylate synthase. |
Duquesne University |
| 8164249 |
46 |
Application of the three-dimensional structures of protein target molecules in structure-based drug design. |
Abbott Laboratories |
| 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 |
| 2642553 |
5 |
Rational design of enzyme inhibitors: multisubstrate analogue inhibitors. |
University of Utah |
| 3373483 |
39 |
Linear free energy relationship studies of enzyme active site binding: thymidylate synthase. |
University of Kansas |
| 3184122 |
10 |
A pyrimidine-based"flexible" bisubstrate analogue inhibitor of human thymidylate synthase. |
University of Utah |
| 3470522 |
16 |
Folate analogues as inhibitors of thymidylate synthase. |
TBA |
| 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 |
| 6502602 |
9 |
A potent multisubstrate analogue inhibitor of human thymidylate synthetase. |
TBA |
| 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 |
| 21696158 |
50 |
Identification of the binding modes of N-phenylphthalimides inhibiting bacterial thymidylate synthase through X-ray crystallography screening. |
Universita Degli Studi Di Modena E Reggio Emilia |
| 21080724 |
57 |
Analogues of 4-[(7-Bromo-2-methyl-4-oxo-3H-quinazolin-6-yl)methylprop-2-ynylamino]-N-(3-pyridylmethyl)benzamide (CB-30865) as potent inhibitors of nicotinamide phosphoribosyltransferase (Nampt). |
Myrexis |
| 20951595 |
1 |
Ligand-based virtual screening and ADME-tox guided approach to identify triazolo-quinoxalines as folate cycle inhibitors. |
Università |
| 20527892 |
7 |
Novel approaches for targeting thymidylate synthase to overcome the resistance and toxicity of anticancer drugs. |
Institute of Theoretical Studies Ggmbh |
| 20163895 |
1 |
Synthesis of new pyrrolo[2,3-d]pyrimidine derivatives and evaluation of their activities against human colon cancer cell lines. |
University College of Pharmaceutical Sciences |
| | 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 |
| 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 |
| 15715461 |
18 |
Improving specificity vs bacterial thymidylate synthases through N-dansyl modulation of didansyltyrosine. |
Università |
| 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 |
| 10377234 |
12 |
Synthesis of classical and a nonclassical 2-amino-4-oxo-6-methyl-5-substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitors of thymidylate synthase. |
Duquesne 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 |
| 9057854 |
41 |
Structure-based design of substituted diphenyl sulfones and sulfoxides as lipophilic inhibitors of thymidylate synthase. |
Agouron Pharmaceuticals |
| 8459400 |
74 |
Design of thymidylate synthase inhibitors using protein crystal structures: the synthesis and biological evaluation of a novel class of 5-substituted quinazolinones. |
Agouron Pharmaceuticals |
| 8360872 |
3 |
Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some 3-amino- and 3-methylbenzo[f]quinazolin-1(2H)-ones. |
Wellcome Research Laboratories |
| 8230138 |
15 |
Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some sulfonamidobenzoylglutamate and related derivatives. |
Wellcome Research Laboratories |
| 8164259 |
44 |
Classical and nonclassical furo[2,3-d]pyrimidines as novel antifolates: synthesis and biological activities. |
Duquesne University |
| 8145235 |
9 |
Benzo[f]quinazoline inhibitors of thymidylate synthase: methyleneamino-linked aroylglutamate derivatives. |
Wellcome Research Laboratories |
| 7783121 |
20 |
Synthesis and biological evaluation of novel 2,6-diaminobenz[cd]indole inhibitors of thymidylate synthase using the protein structure as a guide. |
Agouron Pharmaceuticals |
| 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 |
| 6434741 |
2 |
Interaction of N4-hydroxy-2'-deoxycytidylic acid with thymidylate synthetase. |
TBA |
| 3746818 |
1 |
Thiol addition to quinones: model reactions for the inactivation of thymidylate synthase by 5-p-benzoquinonyl-2'-deoxyuridine 5'-phosphate. |
TBA |
| 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 |
| 28830032 |
9 |
Novel 6-substituted benzoyl and non-benzoyl straight chain pyrrolo[2,3-d]pyrimidines as potential antitumor agents with multitargeted inhibition of TS, GARFTase and AICARFTase. |
Hebei Medical University |
| 2066965 |
28 |
Design of enzyme inhibitors using iterative protein crystallographic analysis. |
Agouron Pharmaceuticals |
| 1995884 |
4 |
Synthesis and biological activity of 5,11-methylenetetrahydro-5- deazahomofolic acid. |
Duquesne University |
| 1995868 |
4 |
The renewed potential for folate antagonists in contemporary cancer chemotherapy. |
Parke-Davis Pharmaceutical Research Division |
| 1732551 |
6 |
Synthesis and antifolate evaluation of the 10-propargyl derivatives of 5-deazafolic acid, 5-deazaaminopterin, and 5-methyl-5-deazaaminopterin. |
Southern Research Institute |
| 1548676 |
28 |
Design and synthesis of novel 6,7-imidazotetrahydroquinoline inhibitors of thymidylate synthase using iterative protein crystal structure analysis. |
Agouron Pharmaceuticals |
| 1433179 |
13 |
5,10-Methylenetetrahydro-5-deazafolic acid and analogues: synthesis and biological activities. |
Duquesne University |
| 9247853 |
7 |
Yeast hexokinase inhibitors designed from the 3-D enzyme structure rebuilding. |
Universite Paul Sabatier |
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