(Q40634281)

English

Design, synthesis, and biological evaluation of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase

scientific article published on October 2003

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scholarly article

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

Design, synthesis, and biological evaluation of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase (English)

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

1 reference

based on heuristic

inferred from title

Ian Andrew Wilson

6

object named as

Ian A Wilson

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

author name string

Thomas H Marsilje

1

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

Michael P Hedrick

2

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

Joel Desharnais

3

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

Ali Tavassoli

4

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

Yan Zhang

5

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

Stephen J Benkovic

7

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

Dale L Boger

8

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

language of work or name

0 references

publication date

1 October 2003

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

Bioorganic & Medicinal Chemistry

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

11

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

20

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

4487-4501

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

The transformylase enzymes of de novo purine biosynthesis

1 reference

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Structural features of 5,10-dideaza-5,6,7,8-tetrahydrofolate that determine inhibition of mammalian glycinamide ribonucleotide formyltransferase

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7 January 2021

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N10-substituted 5,8-dideazafolate inhibitors of glycinamide ribonucleotide transformylase

1 reference

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Synthesis and antitumor activity of 5-deaza-5,6,7,8-tetrahydrofolic acid and its N10-substituted analogues

1 reference

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7 January 2021

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Synthesis and biological activity of an acyclic analogue of 5,6,7,8-tetrahydrofolic acid, N-[4-[[3-(2,4-diamino-1,6-dihydro-6-oxo-5- pyrimidinyl)propyl]amino]-benzoyl]-L-glutamic acid

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Synthesis and biological activity of open-chain analogues of 5,6,7,8-tetrahydrofolic acid--potential antitumor agents

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A dideazatetrahydrofolate analogue lacking a chiral center at C-6, N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5- yl)ethyl]benzoyl]-L-glutamic acid, is an inhibitor of thymidylate synthase

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Synthesis and antifolate evaluation of 10-ethyl-5-methyl-5,10- dideazaaminopterin and an alternative synthesis of 10-ethyl-10- deazaaminopterin (edatrexate)

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7 January 2021

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Synthesis and biological activity of acyclic analogues of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid

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Design and synthesis of inhibitors of folate-dependent enzymes as antitumor agents.

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7 January 2021

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Analogues of 10-deazaaminopterin and 5-alkyl-5,10-dideazaaminopterin with the 4-substituted 1-naphthoyl group in the place of 4-substituted benzoyl

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Protein structure-based design, synthesis, and biological evaluation of 5-thia-2,6-diamino-4(3H)-oxopyrimidines: potent inhibitors of glycinamide ribonucleotide transformylase with potent cell growth inhibition

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7 January 2021

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Multiple folate enzyme inhibition: mechanism of a novel pyrrolopyrimidine-based antifolate LY231514 (MTA).

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7 January 2021

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A multisubstrate adduct inhibitor of AICAR transformylase

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7 January 2021

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The synthesis and biological activity of a series of 2,4-diaminopyrido[2,3-d]pyrimidine based antifolates as antineoplastic and antiarthritic agents

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7 January 2021

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Synthesis and biological activity of 4-amino-7-oxo-substituted analogues of 5-deaza-5,6,7,8-tetrahydrofolic acid and 5,10-dideaza-5, 6,7,8-tetrahydrofolic acid

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7 January 2021

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Phase I study of AG2034, a targeted GARFT inhibitor, administered once every 3 weeks

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7 January 2021

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Synthesis and biological activity of 7-oxo substituted analogues of 5-deaza-5,6,7,8-tetrahydrofolic acid (5-DATHF) and 5,10-dideaza-5,6,7,8-tetrahydrofolic acid (DDATHF).

1 reference

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7 January 2021

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Phase I study of (6R)-5,10-dideazatetrahydrofolate: a folate antimetabolite inhibitory to de novo purine synthesis

1 reference

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7 January 2021

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A phase I clinical study of the antipurine antifolate lometrexol (DDATHF) given with oral folic acid.

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7 January 2021

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Weekly lometrexol with daily oral folic acid is appropriate for phase II evaluation

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7 January 2021

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Phase I and pharmacokinetic study of LY309887: a specific inhibitor of purine biosynthesis

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7 January 2021

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AG2034: a novel inhibitor of glycinamide ribonucleotide formyltransferase

1 reference

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7 January 2021

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Phase I dose-escalation and pharmacokinetic study of a novel folate analogue AG2034

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7 January 2021

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Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 2. Effect of varying the heterocyclic ring on in vitro potency

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Synthesis and structure-activity relationships of peptidyl alpha-keto heterocycles as novel inhibitors of prolyl endopeptidase

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Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles

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Potent thrombin inhibitors that probe the S1 subsite: tripeptide transition state analogues based on a heterocycle-activated carbonyl group

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Peptidomimetic inhibitors of the human cytomegalovirus protease.

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Inhibition of human neutrophil elastase. 4. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of P2-modified, orally active peptidyl pentafluoroethyl ketones

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Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors

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Development of orally active nonpeptidic inhibitors of human neutrophil elastase.

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Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors

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Exceptionally potent inhibitors of fatty acid amide hydrolase: the enzyme responsible for degradation of endogenous oleamide and anandamide

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7 January 2021

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alpha-Keto heterocycle inhibitors of fatty acid amide hydrolase: carbonyl group modification and alpha-substitution

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1 reference

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7 January 2021

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10-Formyl-5,8,10-trideazafolic acid (10-formyl-TDAF): a potent inhibitor of glycinamide ribonucleotide transformylase

1 reference

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Functionalized analogues of 5,8,10-trideazafolate as potential inhibitors of GAR Tfase or AICAR Tfase

1 reference

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7 January 2021

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Functionalized analogues of 5,8,10-trideazafolate: development of an enzyme-assembled tight binding inhibitor of GAR Tfase and a potential irreversible inhibitor of AICAR Tfase

1 reference

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Abenzyl 10-formyl-trideazafolic acid (abenzyl 10-formyl-TDAF): an effective inhibitor of glycinamide ribonucleotide transformylase

1 reference

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Multisubstrate analogue based on 5,8,10-trideazafolate

1 reference

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Design, synthesis, and evaluation of potential GAR and AICAR transformylase inhibitors.

1 reference

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7 January 2021

based on heuristic

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Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase

1 reference

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7 January 2021

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1 reference

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1 reference

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1 reference

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7 January 2021

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1 reference

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7 January 2021

based on heuristic

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Induction of HL-60 leukemia cell differentiation by tetrahydrofolate inhibitors of de novo purine nucleotide biosynthesis

1 reference

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7 January 2021

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In vivo antitumor activity and metabolism of a series of 5-deazaacyclotetrahydrofolate (5-DACTHF) analogues

1 reference

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7 January 2021

based on heuristic

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Effect of purine synthesis inhibition on WiDr spheroids in vitro or on WiDr or colon 38 tumors in vivo. Complete growth inhibition but not regression.

1 reference

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7 January 2021

based on heuristic

inferred from DOI database lookup

Crystal structures of human GAR Tfase at low and high pH and with substrate beta-GAR

1 reference

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7 January 2021

based on heuristic

inferred from DOI database lookup

Identifiers

10.1016/S0968-0896(03)00456-5

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

PubMed publication ID

1 reference

Europe PubMed Central

PubMed publication ID

22 September 2017

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