Assay ID | Title | Year | Journal | Article |
AID165909 | Cytostatic activity against proliferation of Raji/TK cells (deoxythymidine kinase deficient Raji cells) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
| Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates. |
AID212663 | Compound was evaluated for the inhibition of L1210 Thymidylate synthase | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID18726 | Apparent rate constant Kon for inactivation of dTMP synthase. | 1984 | Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
| Synthesis and biological activity of 5-fluoro-2',3'-dideoxy-3'-fluorouridine and its 5'-phosphate. |
AID1304932 | Drug uptake in Sprague-Dawley rat liver S9 fraction treated with (S)-Isopropyl 2-(((R)-(((2R,3S,5R)-5-(5-fluoro-2,4-dioxo 3,4-dihydropyrimidin-1(2H)-yl)-3-hydroxytetrahydrofuran-2-yl)methoxy)((2-methylbenzyl)oxy)phosphoryl)amino)propanoate at 20 ug/mL pre | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of an Orally Active and Liver-Targeted Prodrug of 5-Fluoro-2'-Deoxyuridine for the Treatment of Hepatocellular Carcinoma. |
AID85714 | Antiviral activity against Herpes Simplex Virus-1 (McIntyre) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
| Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates. |
AID230651 | Ki/Km values of L1210/0 dTMP synthase for the compound was determined. | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
| Synthesis and biological properties of some cyclic phosphotriesters derived from 2'-deoxy-5-fluorouridine. |
AID212635 | Inhibition of cellular thymidylate synthase activity of murine leukemia cell line (L1210) in permeabilised cells. | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
| Synthesis and biological activity of aromatic amino acid phosphoramidates of 5-fluoro-2'-deoxyuridine and 1-beta-arabinofuranosylcytosine: evidence of phosphoramidase activity. |
AID211051 | Affinity towards thymidine monophosphate kinase (TMPKmt) in Mycobacterium tuberculosis | 2003 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 13, Issue:18
| Thymidine and thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase. |
AID96658 | Dose inhibiting L1210/0 murine leukemia cell proliferation by 50% in presence of 5 ug/mL of dThd. | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
| Synthesis and biological properties of some cyclic phosphotriesters derived from 2'-deoxy-5-fluorouridine. |
AID211054 | Kinetic parameter Vm of thymidine monophosphate kinase (TMPKmt) in Mycobacterium tuberculosis was determined | 2003 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 13, Issue:18
| Thymidine and thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase. |
AID96642 | Cytostatic activity against proliferation of L1210/0 cells (murine leukemia L1210 cells) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
| Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates. |
AID229760 | Ratio of ID50 upon addition of dThd to the ID50 upon addition of dUrd against the L1210/0 cell proliferation. | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
| Synthesis and biological properties of some cyclic phosphotriesters derived from 2'-deoxy-5-fluorouridine. |
AID1134942 | Competitive inhibition of thymidylate synthase purified from methotrexate-resistant Lactobacillus casei using 2'-deoxy[5-3H]uridine 5'-phosphate by radioisotope assay | 1979 | Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
| 5-Cyano-2'-deoxyuridine 5'-phosphate: a potent competitive inhibitor of thymidylate synthetase. |
AID87506 | Evaluation of antiviral activity against Herpes simplex virus type 1 (HSV-1) strain F | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID87508 | Evaluation of antiviral activity against Herpes simplex virus type 1 (HSV-1) strain McIntyre | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID220363 | Binding of 0.1 mM [14C]5,10-CH2-H4 folate to 2.5 nmol dTMP synthetase from Lactobacillus casei | 1981 | Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
| Interaction of 5-ethynyl-2'-deoxyuridylate with thymidylate synthetase. |
AID87507 | Evaluation of antiviral activity against Herpes simplex virus type 1 (HSV-1) strain KOS. | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID211240 | The time dependent reaction (k2''(1/min)) of compound was measured for inactivation of Ehrlich Carcinoma Thymidylate Synthases | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
| 2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID87828 | Evaluation of antiviral activity against Herpes simplex virus type 2 (HSV-2) strain Lyons | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID232972 | Ratio of Concentration of intact versus pearmeabilized of above | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
| Synthesis and biological activity of aromatic amino acid phosphoramidates of 5-fluoro-2'-deoxyuridine and 1-beta-arabinofuranosylcytosine: evidence of phosphoramidase activity. |
AID211241 | The time dependent reaction (k2''(1/min)) of compound was measured for inactivation of L1210 Thymidylate Synthases | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
| 2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID221339 | Evaluation for antitumor activity against human lymphoblast Raji cells | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID1147598 | Binding affinity to amethopterin-resistant Lactobacillus casei thymidylate synthetase in presence of cofactor not permitting covalent bond formation | 1977 | Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
| Inhibition of Lactobacillus casei thymidylate synthetase by 5-substituted 2'-deoxyuridylates. Preliminary quantitative structure-activity relationship. |
AID704506 | Ratio of IC50 for human CEM cells expressing human ENT1 transporter in presence of dipyridamole to IC50 for human CEM cells expressing human ENT1 transporter | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Phosphoramidate ProTides of the anticancer agent FUDR successfully deliver the preformed bioactive monophosphate in cells and confer advantage over the parent nucleoside. |
AID211056 | Compound was tested for binding affinity against Mycobacterium tuberculosis thymidine monophosphate kinase | 2002 | Bioorganic & medicinal chemistry letters, Oct-07, Volume: 12, Issue:19
| Synthesis and evaluation of thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase. |
AID216408 | Antiviral activity against vesicular stomatitis virus | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
| Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates. |
AID87826 | Evaluation of antiviral activity against Herpes simplex virus type 2 (HSV-2) strain 196. | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID228255 | Compound was tested for time-dependent slow-binding inhibition (K) of thymidylate synthase from L1210-P cells | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| 5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID228416 | Compound was tested for time-dependent 1 (k2) inhibition of thymidylate synthase from L1210-R cells | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| 5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID1147597 | Binding affinity to amethopterin-resistant Lactobacillus casei thymidylate synthetase in presence of cofactor permitting covalent bond formation | 1977 | Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
| Inhibition of Lactobacillus casei thymidylate synthetase by 5-substituted 2'-deoxyuridylates. Preliminary quantitative structure-activity relationship. |
AID211238 | The reaction rate(Ki'') of compound was measured for inactivation of L1210 Thymidylate Synthases | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
| 2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID23991 | Half-life period of [6-3H]3''-FFdUMP from its ternary complex with dTMP synthetase. | 1984 | Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
| Synthesis and biological activity of 5-fluoro-2',3'-dideoxy-3'-fluorouridine and its 5'-phosphate. |
AID220356 | Compound was evaluated for the inhibition of dTMP synthetase with respect to dUMP. | 1981 | Journal of medicinal chemistry, Oct, Volume: 24, Issue:10
| Interaction of 1-(5-phospho-beta-D-arabinofuranosyl)-5-substituted-uracils with thymidylate synthetase: mechanism-based inhibition by 1-(5-phospho-beta-D-arabinosyl)-5-fluorouracil. |
AID98529 | Evaluation of antitumor activity against mutant murine leukemia L1210 cells | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID217995 | Antiviral activity against vaccinia virus | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
| Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates. |
AID228256 | Compound was tested for time-dependent slow-binding inhibition (K) of thymidylate synthase from L1210-R cells | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| 5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID704505 | Ratio of IC50 for human CEM cells expressing human ENT1 transporter in presence of NBMPR to IC50 for human CEM cells expressing human ENT1 transporter | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Phosphoramidate ProTides of the anticancer agent FUDR successfully deliver the preformed bioactive monophosphate in cells and confer advantage over the parent nucleoside. |
AID96655 | Dose inhibiting L1210/0 murine leukemia cell proliferation by 50% | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
| Synthesis and biological properties of some cyclic phosphotriesters derived from 2'-deoxy-5-fluorouridine. |
AID96656 | Dose inhibiting L1210/0 murine leukemia cell proliferation by 50% in presence of 125 ug/mL of dUrd. | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
| Synthesis and biological properties of some cyclic phosphotriesters derived from 2'-deoxy-5-fluorouridine. |
AID228258 | Compound was tested for time-dependent 1 (k2') inhibition of thymidylate synthase from L1210-R cells | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| 5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID85713 | Antiviral activity against Herpes Simplex Virus-1 (KOS) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
| Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates. |
AID220371 | In vitro competitive inhibition of cleavage of substrate dUMP phosphorylase. | 1984 | Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
| Synthesis and biological activity of 5-fluoro-2',3'-dideoxy-3'-fluorouridine and its 5'-phosphate. |
AID1321552 | Inhibition of Mycobacterium tuberculosis ThyX at 100 uM preincubated with enzyme followed by [5-3H]dUMP substrate addition measured after 30 mins in presence of 5,10-methylenetetrahydrofolate,NADPH and FAD by liquid scintillation counting | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Virtual Screening and X-ray Crystallography Identify Non-Substrate Analog Inhibitors of Flavin-Dependent Thymidylate Synthase. |
AID704507 | Ratio of IC50 for ENT1 transporter-deficient human CEM cells to IC50 for human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Phosphoramidate ProTides of the anticancer agent FUDR successfully deliver the preformed bioactive monophosphate in cells and confer advantage over the parent nucleoside. |
AID99522 | In vitro percent inhibition at 10 e-8 M against L5178Y cell growth after 72 hr (replicate flasks inoculated with 10 e5 cells were treated with the nucleotide) | 1980 | Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
| Synthesis and biological activity of 5-fluoro-2'-deoxyuridine 5'-phosphorodiamidates. |
AID704508 | Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting in presence of NBMPR | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Phosphoramidate ProTides of the anticancer agent FUDR successfully deliver the preformed bioactive monophosphate in cells and confer advantage over the parent nucleoside. |
AID1147592 | Inhibition of amethopterin-resistant Lactobacillus casei thymidylate synthetase-catalyzed dTMP formation using dUMP as substrate by spectrophotometric analysis in presence of CH2-H4-folate | 1977 | Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
| Inhibition of Lactobacillus casei thymidylate synthetase by 5-substituted 2'-deoxyuridylates. Preliminary quantitative structure-activity relationship. |
AID211088 | The reaction rate(Ki') of compound was measured for inactivation of Ehrlich Carcinoma Thymidylate Synthases | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
| 2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID17052 | Apparent rate constant Koff for inactivation of dTMP synthase. | 1984 | Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
| Synthesis and biological activity of 5-fluoro-2',3'-dideoxy-3'-fluorouridine and its 5'-phosphate. |
AID96659 | Dose inhibiting L1210/Br-dUrd murine leukemia cell proliferation by 50% | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
| Synthesis and biological properties of some cyclic phosphotriesters derived from 2'-deoxy-5-fluorouridine. |
AID704510 | Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Phosphoramidate ProTides of the anticancer agent FUDR successfully deliver the preformed bioactive monophosphate in cells and confer advantage over the parent nucleoside. |
AID709346 | Inhibition of human thymidylate synthase expressed in Escherichia coli incubated for 1 hr by spectrophotometry | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Inhibitor of ovarian cancer cells growth by virtual screening: a new thiazole derivative targeting human thymidylate synthase. |
AID212496 | Inhibition of cellular thymidylate synthase activity of mouse fibroblast (L929 TK-) in intact cells. | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
| Synthesis and biological activity of aromatic amino acid phosphoramidates of 5-fluoro-2'-deoxyuridine and 1-beta-arabinofuranosylcytosine: evidence of phosphoramidase activity. |
AID1147594 | Inhibition of amethopterin-resistant Lactobacillus casei thymidylate synthetase-catalyzed 5-BrdUMP dehalogenation by absorbance analysis in absence of CH2-H4-folate | 1977 | Journal of medicinal chemistry, Nov, Volume: 20, Issue:11
| Inhibition of Lactobacillus casei thymidylate synthetase by 5-substituted 2'-deoxyuridylates. Preliminary quantitative structure-activity relationship. |
AID98532 | Evaluation of cytostatic activity by using antitumor assays against murine leukemia L1210 cells | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID229757 | Ratio of ID50 for L1210/0 cell growth and ID50 for L1210/BdUrd cell growth. | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
| Synthesis and biological properties of some cyclic phosphotriesters derived from 2'-deoxy-5-fluorouridine. |
AID216539 | Evaluation of antiviral activity against Vesicular stomatitis virus. | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID218132 | Evaluation of antiviral activity against Vaccinia virus | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID84761 | Antiviral activity against Herpes Simplex Virus-2(G) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
| Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates. |
AID228252 | Time-independent inhibition of thymidylate synthase from parenteral L1210 cells | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| 5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID211245 | The time dependent reaction (k2'(1/min)) of compound was measured for inactivation of L1210 Thymidylate Synthases | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
| 2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID98737 | In vitro cytotoxicity of compounds were determined on murine leukemia cell line (L1210). | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
| Synthesis and biological activity of aromatic amino acid phosphoramidates of 5-fluoro-2'-deoxyuridine and 1-beta-arabinofuranosylcytosine: evidence of phosphoramidase activity. |
AID43713 | In vitro cytotoxicity of compounds were determined on Inhibition of human leukemia cell line(CCRF-CEM). | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
| Synthesis and biological activity of aromatic amino acid phosphoramidates of 5-fluoro-2'-deoxyuridine and 1-beta-arabinofuranosylcytosine: evidence of phosphoramidase activity. |
AID220992 | Evaluation of antitumor activity against thymidine kinase deficient Raji cell line | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID211236 | The reaction rate(Ki'') of compound was measured for inactivation of Ehrlich Carcinoma Thymidylate Synthases | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
| 2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID96643 | Cytostatic activity against proliferation of L1210/BdU cells (deoxythymidine kinase deficient L1210 cells) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
| Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates. |
AID233941 | Ratio between Ki of L1210-P enzyme and Michaelis-Menten constant (kM) | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| 5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID228254 | Compound was tested for time-dependent slow-binding inhibition (K') of thymidylate synthase from L1210-R cells | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| 5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID680603 | TP_TRANSPORTER: transport into inside-out membrane vesicles in membrane vesicle from MRP8-2-expressing LLC-PK1 cells | 2003 | The Journal of biological chemistry, Aug-08, Volume: 278, Issue:32
| MRP8, ATP-binding cassette C11 (ABCC11), is a cyclic nucleotide efflux pump and a resistance factor for fluoropyrimidines 2',3'-dideoxycytidine and 9'-(2'-phosphonylmethoxyethyl)adenine. |
AID211811 | Compound was tested for its inhibition against Thymidylate synthase up to concentration of 1 mM; IA means inactive | 1980 | Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
| Synthesis and biological activity of 5-fluoro-2'-deoxyuridine 5'-phosphorodiamidates. |
AID84760 | Antiviral activity against Herpes Simplex Virus-2(196) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
| Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates. |
AID1123575 | Inhibition of Lactobacillus casei thymidylate synthetase using dUMP as substrate without pre-incubation with enzyme at 1.2 X 10'-7 M relative to control | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
| Phosphonate analogue of 2'-deoxy-5-fluorouridylic acid. |
AID704509 | Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting in presence of dipyridamole | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Phosphoramidate ProTides of the anticancer agent FUDR successfully deliver the preformed bioactive monophosphate in cells and confer advantage over the parent nucleoside. |
AID228251 | Time-independent inhibition of thymidylate synthase from FdUrd-resistant L1210 cells | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| 5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID211244 | The time dependent reaction (k2'(1/min)) of compound was measured for inactivation of Ehrlich Carcinoma Thymidylate Synthases | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
| 2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID99399 | Inhibitory activity against Lactobacillus casei MTX-resistant | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
| 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). |
AID211057 | Enzyme Kinetic constant was determined in the presence of Mycobacterium tuberculosis thymidine monophosphate kinase | 2002 | Bioorganic & medicinal chemistry letters, Oct-07, Volume: 12, Issue:19
| Synthesis and evaluation of thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase. |
AID228253 | Compound was tested for time-dependent slow-binding inhibition (K') of thymidylate synthase from L1210-P cells | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| 5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID704511 | Cytostatic activity against ENT1 transporter-deficient human CEM cells after 72 hrs by cell counting | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Phosphoramidate ProTides of the anticancer agent FUDR successfully deliver the preformed bioactive monophosphate in cells and confer advantage over the parent nucleoside. |
AID212499 | Inhibition of cellular thymidylate synthase activity of murine leukemia cell line (L1210) in intact cells. | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
| Synthesis and biological activity of aromatic amino acid phosphoramidates of 5-fluoro-2'-deoxyuridine and 1-beta-arabinofuranosylcytosine: evidence of phosphoramidase activity. |
AID228257 | Compound was tested for time-dependent 1 (k2') inhibition of thymidylate synthase from L1210-P cells | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| 5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID211086 | Apparent Ki value was measured by competitive inhibition of Thymidylate Synthases from Ehrlich Carcinoma cells of mouse | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
| 2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID87827 | Evaluation of antiviral activity against Herpes simplex virus type 2 (HSV-2) strain G | 1986 | Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
| Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neutral triesters. |
AID165908 | Cytostatic activity against proliferation of Raji/0 cells (human lymphoblast Raji cells) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
| Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates. |
AID211087 | Apparent Ki value was measured by competitive inhibition of Thymidylate Synthases from L1210 cells of mouse | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
| 2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID84762 | Antiviral activity against Herpes Simplex Virus-2(Lyons) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
| Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates. |
AID211090 | The reaction rate(Ki') of compound was measured for inactivation of L1210 Thymidylate Synthases | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
| 2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID233942 | Ratio between Ki of L1210-R enzyme and Michaelis-Menten constant (kM) | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| 5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
AID99823 | In vitro cytotoxicity of compounds were determined on mouse fibroblast (L929 TK-). | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
| Synthesis and biological activity of aromatic amino acid phosphoramidates of 5-fluoro-2'-deoxyuridine and 1-beta-arabinofuranosylcytosine: evidence of phosphoramidase activity. |
AID85712 | Antiviral activity against Herpes Simplex Virus-1 (F) | 1986 | Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
| Synthesis, structure, and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates. |
AID212498 | Inhibition of cellular thymidylate synthase activity of mouse fibroblast (L929 TK-) in permeabilised cells. | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
| Synthesis and biological activity of aromatic amino acid phosphoramidates of 5-fluoro-2'-deoxyuridine and 1-beta-arabinofuranosylcytosine: evidence of phosphoramidase activity. |
AID99514 | Comparative inhibition of L5178Y cell growth in vitro (concentration required for 50% inhibition) | 1980 | Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
| Synthesis and biological activity of 5-fluoro-2'-deoxyuridine 5'-phosphorodiamidates. |
AID228415 | Compound was tested for time-dependent 1 (k2) inhibition of thymidylate synthase from L1210-P cells | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| 5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |