PMID

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Article Title

Organization

The effect of 5-substitution in the pyrimidine ring of dUMP on the interaction with thymidylate synthase: molecular modeling and QSAR.

Polish Academy Of Sciences

Folate-based inhibitors of thymidylate synthase: synthesis and antitumor activity of gamma-linked sterically hindered dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).

The Institute Of Cancer Research

Syntheses and thymidylate synthase inhibitory activity of the poly-gamma-glutamyl conjugates of N-[5-[N-(3,4-dihydro-2-methyl-4-oxoquinazolin-6-ylmethyl)-N-methylamino ]-2-thenoyl]-L-glutamic acid (ICI D1694) and other quinazoline antifolates.

Institute Of Cancer Research

Cyclopenta[g]quinazoline-based antifolates: the effect of the chirality at the 6-position on the inhibition of thymidylate synthase (TS).

The Institute Of Cancer Research

5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity.

Polish Academy Of Sciences

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

The synthesis and thymidylate synthase inhibitory activity of L-gamma-L-linked dipeptide and L-gamma-amide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).

Institute Of Cancer Research

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.

Princeton University

Quinoline antifolate thymidylate synthase inhibitors: variation of the C2- and C4-substituents.

Ici Pharmaceuticals Group

Quinazoline antifolate thymidylate synthase inhibitors: heterocyclic benzoyl ring modifications.

Ici Pharmaceuticals Group

Potent inhibition of thymidylate synthase by two series of nonclassical quinazolines.

Warner-Lambert

Linear free energy relationship studies of enzyme active site binding: thymidylate synthase.

University Of Kansas

Folate analogues as inhibitors of thymidylate synthase.

TBA

Folate analogues. 25. Synthesis and biological evaluation of N10-propargylfolic acid and its reduced derivatives.

TBA

Synthesis and biological evaluation of unsaturated keto and exomethylene D-arabinopyranonucleoside analogs: novel 5-fluorouracil analogs that target thymidylate synthase.

University Of Thessaly

 

Carboxylic acid bioisosteres of γ-linked dipeptide analogues of the folate-based thymidylate synthase (TS) inhibitor, 2-desamino-2-methyl-N¹⁰-propargyl-5,8-dideazafolic acid (ICI 198583)

TBA

The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent.

The Institute Of Cancer Research

Synthesis and biological studies of novel nucleoside phosphoramidate prodrugs.

Purdue University

Design and synthesis of Cyclopenta[g]quinazoline-based antifolates as inhibitors of thymidylate synthase and potential antitumor agents(,).

The Institute Of Cancer Research

Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors.

Astrazeneca

Quinazoline antifolates thymidylate synthase inhibitors: lipophilic analogues with modification to the C2-methyl substituent.

Zeneca Pharma

Quinazoline antifolate thymidylate synthase inhibitors: gamma-linked L-D, D-D, and D-L dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).

Institute Of Cancer Research

2-Thio derivatives of dUrd and 5-fluoro-dUrd and their 5'-monophosphates: synthesis, interaction with tumor thymidylate synthase, and in vitro antitumor activity.

Polish Academy Of Sciences

Quinazoline antifolate thymidylate synthase inhibitors: replacement of glutamic acid in the C2-methyl series.

Zeneca Pharmaceuticals

Inhibition by 5-(substituted-benzyl)-2,4-diaminopyrimidines of murine tumor (L5178Y) cell cultures sensitive to and resistant to methotrexate. Further evidence for the sensitivity of resistant cells to hydrophobic drugs.

TBA

Quinazoline antifolates inhibiting thymidylate synthase: variation of the N10 substituent.

TBA

Quinazoline antifolates inhibiting thymidylate synthase: benzoyl ring modifications.

TBA

Folate analogues. 30. Synthesis and biological evaluation of N10-propargyl-5,8-dideaza-5,6,7,8-tetrahydrofolic acid and related compounds.

TBA

5-Quinone derivatives of 2'-deoxyuridine 5'-phosphate: inhibition and inactivation of thymidylate synthase, antitumor cell, and antiviral studies.

TBA

Quinazoline antifolates inhibiting thymidylate synthase: 2-desamino derivatives with enhanced solubility and potency.

Institute Of Cancer Research

Quinazoline antifolate thymidylate synthase inhibitors: benzoyl ring modifications in the C2-methyl series.

Ici Pharmaceuticals Group

Quinazoline antifolate thymidylate synthase inhibitors: 2'-fluoro-N10-propargyl-5,8-dideazafolic acid and derivatives with modifications in the C2 position.

Institute Of Cancer Research

Quinazoline antifolate thymidylate synthase inhibitors: alkyl, substituted alkyl, and aryl substituents in the C2 position.

Ici Pharmaceuticals Group

Quinazoline antifolate thymidylate synthase inhibitors: bridge modifications and conformationally restricted analogues in the C2-methyl series.

Ici Pharmaceuticals Group

Quinazoline antifolates inhibiting thymidylate synthase: 4-thio-substituted analogues.

Institute Of Cancer Research

N-[4-[[(3,4-dihydro-4-oxo-1,2,3-benzotriazin-6- yl)methyl]amino]benzoyl]-L-glutamic acid, a novel A-ring analogue of 2-desamino-5,8-dideazafolic acid.

Harvard Medical School

Quinazoline antifolate thymidylate synthase inhibitors: difluoro-substituted benzene ring analogues.

Institute Of Cancer Research