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(2S)-2-(((5-(2-((6R)-2-amino-4-oxo-5,6,7,8-tetrahydro-1H-pyrido[2,3-d]-pyrimidin-6-yl)ethyl)thiophene-2-yl)carbonyl)amino)-pentanedioic acid
LY309887
(2S)-2-(((5-(2-((6S)-2-amino-4-oxo-1,6,7,8-tetrahydropyrimido[5,4-b]-[1,4]thiazin-6-yl)ethyl)thiophene-2-yl)carbonyl)amino)-pentanedioic acid
AG2034
(2S)-2-[[4-[(1RS)-1-[(2,4-diaminopteridin-6-yl)methyl]but-3-ynyl]benzoyl]amino]pentanedioic acid
-
(6R)-5,10-dideazatetrahydrofolate
-
lometrexol
(6R)-dideazatetrahydrofolate diglutamate
(6R)-dideazatetrahydrofolate pentaglutamate
(6R)-dideazatetrahydrofolate tetraglutamate
(6R)-dideazatetrahydrofolate triglutamate
(6S)-dideazatetrahydrofolate
(6S)-N10-formyltetrahydrofolate
-
-
(alpha,beta)-hydroxyacetamide ribonucleotide
-
-
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
-
-
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
-
-
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
-
-
(S)-2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)pentanedioic acid
-
(S)-2-(4-(2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzamido)pentanedioic acid
-
(S)-2-(4-(2-(3-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)propyl)-1,3-dithian-2-yl)benzamido)pentanedioic acid
-
-
(S)-2-(4-(3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)propyl)benzamido)pentanedioic acid
-
(S)-2-(4-(4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)butyl)benzamido)pentanedioic acid
-
(S)-2-(4-(5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)pentyl)benzamido)pentanedioic acid
-
(S)-2-(4-(6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)hexyl)benzamido)pentanedioic acid
-
(S)-2-(5-(3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)propyl)thiophene-2-carboxamido)pentanedioic acid
-
(S)-2-(5-(4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)butyl)thiophene-2-carboxamido)pentanedioic acid
-
(S)-2-(5-(5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)pentyl)thiophene-2-carboxamido)pentanedioic acid
-
(S)-2-(5-(6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)hexyl)thiophene-2-carboxamido)pentanedioic acid
lometrexol, LMTX
(S)-2-[2-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo [2,3-d]pyrimidin-6-yl)-acetylamino]-acetylamino]-pentanedioic acid
-
-
(S)-2-[3-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo [2,3-d]pyrimidin-6-yl)-acetylamino]-propionylamino]-pentanedioic acid
-
-
(S)-2-[4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo [2,3-d]pyrimidin-6-yl)-acetylamino]-benzoylamino]-pentanedioic acid
-
-
(S)-2-[4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo [2,3-d]pyrimidin-6-yl)-acetylamino]-butyrylamino]-pentanedioic acid
-
-
(S)-2-[5-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo [2,3-d]pyrimidin-6-yl)-acetylamino]-pentanoylamino]-pentanedioic acid
-
-
(S)-2-[6-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo [2,3-d]pyrimidin-6-yl)-acetylamino]-hexanoylamino]-pentanedioic acid
-
-
1-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetyl]-piperidine-4-carboxylic acid (pyridin-3-ylmethyl)-amide
-
10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid
specifically inhibits recombinant GAR Tfase, inactive against other folate-dependent enzymes, potent inhibitor of tumor cell proliferation
10-Acetyl-5,8-dideazafolate
10-formyl-5,10-dideaza-5,6,7,8-tetrahydrofolic acid
-
10-formyl-5,8-dideazafolic acid hexaglutamate
-
-
10-methanesulfonyl-5-DACTHF
-
-
10-methanesulfonyl-DDACTHF
-
-
10-methylthio-DDACTHF
-
-
10-trifluoroacetyl-DDACTHF
2',3'-dideoxy-2',3'-didehydro-carbocyclic glycinamide ribonucleotide
-
-
2',3'-dideoxy-carbocyclic glycinamide ribonucleotide
-
-
2',5'-furan-dideazatetrahydrofolate
2',5'-thiophene dideazatetrahydrofolate
2,4-diamino-6-(3,4,5-trimethoxyanilino)-methylpyrido[3,2-d]pyrimidine
PY873
2,4-diamino-6-(3,4,5-trimethoxybenzyl)-5,6,7,8-tetrahydro-quinazoline
PY899
2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-N-[[(pyridin-3-ylmethyl)-carbamoyl]-methyl]-acetamide
-
2-deaminodideazatetrahydrofolate
-
-
3-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-N-pyridin-3-ylmethyl-propionamide
-
4-([2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-methyl)-N-pyridin-3-ylmethyl-benzamide
inhibition of thymidylate synthase, as well as glycinamide ribonucleotide formyltransferase and ribonucleotide formyltransferase. Growth inhibition of 4-([2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-methyl)-N-pyridin-3-ylmethyl-benzamide toward KB cells results in cytotoxicity and G1/G2-phase accumulation, and is partially protected by excess thymidine and adenosine, but is completely reversed in the combination of thymidine and adenosine
4-carbamoyl-2-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
4-carbamoyl-4-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-cyclohexanecarboxylic acid (pyridin-3-ylmethyl)-amide
-
4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-N-pyridin-3-ylmethyl-benzamide
-
4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-N-pyridin-3-ylmethyl-butyramide
-
5'-phosphonate carbocyclic glycinamide ribonucleotide
-
-
5,10-dideaza-5,6,7,8-tetrahydrofolate
5,10-dideaza-5,6,7,8-tetrahydrofolic acid
-
-
5,10-dideazafolic acid
-
-
5,10-dideazatetrahydrofolate
5,8-dideazafolate hexaglutamate
-
-
5,8-dideazapteroyl hexaglutamate
-
-
5-((4-carboxy-4-(4-(((2,4-diaminopyrido[3,2-d]pyrimidine-6-yl)methyl)amino)benzamido)butyl)carbamoyl)-isophthalic acid
iDIA
5-deazatetrahydrofolate
-
-
5-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-pentanoic acid (pyridin-3-ylmethyl)-amide
-
6-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)-acetylamino]-hexanoic acid (pyridin-3-ylmethyl)-amide
-
alpha,beta-hydroxyacetamideribonucleotide
-
-
alpha,beta-N-(hydroxyacetyl)-D-ribofuranosylamine
-
-
beta-thioglycinamide dideazafolate
-
-
dideazatetrahydrofolate
-
-
dideazatetrahydrofolate hexaglutamate
-
-
homo-dideazatetrahydrofolate
-
-
L-(+)-10-formyltetrahydrofolate
-
excellent competitive inhibitor
LY231514
-
antitumor activity may result from simultaneous and multiple inhibition of several key folate-requiring enzymes via its polyglutamated metabolites
LY231514 monoglutamate
-
-
LY231514 pentaglutamate
-
-
N-(4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl)-L-glutamic acid
-
N-(4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-propyl]benzoyl)-L-glutamic acid
N-(4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-butyl]benzoyl)-L-glutamic acid
N-(4-[5-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-pentyl]benzoyl)-L-glutamic acid
N-(4-[6-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-hexyl]benzoyl)-L-glutamic acid
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)-gamma-glutamyl-gamma-glutamyl-gamma-glutamyl-gamma-glutamylglutamic acid
-
-
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)-gamma-glutamyl-gamma-glutamylglutamic acid
-
-
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)glutamic acid
-
-
N-(5-[N-(3,4-dihydro-2-methyl-4-oxyquinazolin-6-ylmethyl)-N-methyl-amino]-2-thienoyl)-L-glutamic acid
-
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
-
-
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
-
-
N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
-
-
N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid
N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
N-([5-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2,3-dihydrothiophen-2-yl]carbonyl)-4-methylideneglutamic acid
-
-
N-([5-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophen-2-yl]carbonyl)-L-glutamic acid
-
N-([5-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophen-2-yl]carbonyl)-L-glutamic acid
-
N-[(5-[2-[(6R)-2-amino-4-oxo-3,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin-6-yl]ethyl]-4-methylthiophen-2-yl)carbonyl]glutamic acid
modeling
N-[(5-[2-[(6R)-2-amino-4-oxo-3,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin-6-yl]ethyl]thiophen-2-yl)carbonyl]glutamic acid
modeling
N-[(5-[2-[(6S)-2-amino-4-oxo-4,6,7,8-tetrahydro-3H-pyrimido[5,4-b][1,4]thiazin-6-yl]ethyl]thiophen-2-yl)carbonyl]glutamic acid
modeling
N-[4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]benzoyl]glutamic acid
binding structure analysis, modeling, overview
N-[4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]benzoyl]glutamic acid
binding structure analysis, modeling, overview
N-[4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diaminopyrido[3,2-d]pyrimidin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2-fluorobenzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2-amino-4-methylquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
N-[4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid
N-[4-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid
-
N-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]benzoyl]glutamic acid
-
N-[4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]-L-glutamic acid
-
-
N-[4-[5-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-2-(2,2,2-trifluoroacetyl)pentyl]benzoyl]-L-glutamic acid
-
effective inhibitor
N-[4-[5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl]-L-glutamic acid
-
-
N-[4-[6-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1,1,1-trifluoro-2-oxohexan-3-yl]benzoyl]glutamic acid
-
N-[4-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl]-L-glutamic acid
-
-
N-[5-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]-L-glutamic acid
-
-
N-[5-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]-L-glutamic acid
-
-
N-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexanoyl]-L-glutamic acid
N-[7-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)heptanoyl]-D-glutamic acid
-
-
N-[7-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)heptanoyl]-L-glutamic acid
N-[8-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)octanoyl]-D-glutamic acid
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-
N-{4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl}-L-glutamic acid
-
-
N-{4-[5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl}-L-glutamic acid
-
-
N-{4-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl}-L-glutamic acid
-
-
N10-(Bromoacetyl)-5,8-dideazafolate
-
-
N10-formyl-2,4-diaminodideazafolate
-
-
(6R)-dideazatetrahydrofolate diglutamate
-
LY235340
(6R)-dideazatetrahydrofolate diglutamate
-
LY235340
(6R)-dideazatetrahydrofolate pentaglutamate
-
LY235542
(6R)-dideazatetrahydrofolate pentaglutamate
-
LY235542
(6R)-dideazatetrahydrofolate tetraglutamate
-
LY266978
(6R)-dideazatetrahydrofolate tetraglutamate
-
LY266978
(6R)-dideazatetrahydrofolate triglutamate
-
LY235337
(6R)-dideazatetrahydrofolate triglutamate
-
LY235337
(6S)-dideazatetrahydrofolate
-
LY243246
(6S)-dideazatetrahydrofolate
-
LY243246
10-Acetyl-5,8-dideazafolate
-
-
10-Acetyl-5,8-dideazafolate
-
-
10-Acetyl-5,8-dideazafolate
-
-
10-trifluoroacetyl-DDACTHF
-
-
10-trifluoroacetyl-DDACTHF
-
-
2',5'-furan-dideazatetrahydrofolate
-
LY222306
2',5'-furan-dideazatetrahydrofolate
-
LY222306
2',5'-thiophene dideazatetrahydrofolate
-
LY309887, diastereomer B
2',5'-thiophene dideazatetrahydrofolate
-
LY309886, diastereomer A; LY309887, diastereomer B
2',5'-thiophene dideazatetrahydrofolate
-
LY309887, diastereomer B
2',5'-thiophene dideazatetrahydrofolate
-
LY309886, diastereomer A; LY309887, diastereomer B
4-carbamoyl-2-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
-
-
4-carbamoyl-2-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
-
-
4-carbamoyl-4-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
-
-
4-carbamoyl-4-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
-
-
5,10-dideaza-5,6,7,8-tetrahydrofolate
-
-
5,10-dideaza-5,6,7,8-tetrahydrofolate
-
-
5,10-dideazatetrahydrofolate
-
-
5,10-dideazatetrahydrofolate
-
-
5,10-dideazatetrahydrofolate
-
-
DDACTHF
-
-
lometrexol
i.e. (6R)-5,10-dideaza-5,6,7,8-tetrahydrofolic acid
lometrexol
i.e. 5,10-dideaza-5,6,7,8-tetrahydrofolate
lometrexol
-
i.e. dideazatetrahydrofolate, specific inhibitor
N-(4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-propyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase, resulting in potent growth inhibition of human tumor cells KB and IGROV1 that express folate receptors
N-(4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-propyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase
N-(4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-butyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase, resulting in potent growth inhibition of human tumor cells KB and IGROV1 that express folate receptors
N-(4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-butyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase
N-(4-[5-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-pentyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase, resulting in potent growth inhibition of human tumor cells KB and IGROV1 that express folate receptors
N-(4-[5-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-pentyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase
N-(4-[6-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-hexyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase, resulting in potent growth inhibition of human tumor cells KB and IGROV1 that express folate receptors
N-(4-[6-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-hexyl]benzoyl)-L-glutamic acid
-
dual inhibition of glycinamide ribonucleotide formyltransferase and, likely, 5-amino-4-imidazole carboxamide ribonucleotide formyltransferase
N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid
-
-
N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid
-
-
N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
-
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N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
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N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
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N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
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N-[4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid
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N-[4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid
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N-[4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
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N-[4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
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N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
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N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
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N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
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N-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexanoyl]-L-glutamic acid
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N-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexanoyl]-L-glutamic acid
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N-[7-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)heptanoyl]-L-glutamic acid
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N-[7-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)heptanoyl]-L-glutamic acid
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pemetrexed
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additional information
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10-methanesulfonyl-DDACTHF, 10-methanesulfonyl-5-DACTHF and 10-methylthio-DDACTHF shows KI-values above 0.1 mM
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additional information
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no inhibition by N-[4-[5-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-2-(2,2,2-trifluoroacetyl)pentyl]benzoyl]-L-glutamic acid
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additional information
inhibitor design and evalutaion of cofactor analogues, C10 substitution and stereochemistry, pteridine-binding pocket structure and ligand binding, modeling, overview
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additional information
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inhibitor design and evalutaion of cofactor analogues, C10 substitution and stereochemistry, pteridine-binding pocket structure and ligand binding, modeling, overview
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additional information
synthesis and antitumor activity of a series of 6-substituted pyrrolo[2,3-d]pyrimidines as potential nonclassical antifolates targeting both thymidylate and purine nucleotide biosynthesis, docking study and molecular modeling using the enzyme's crystal structure in complex with compound 10-CF3CO-DDACTHF, PDB ID 1NJS. Growth inhibition of human cancer cells by the inhibitors, IC50 values, overview
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additional information
synthesis of 5-substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitors that acts as a dual inhibitor of GARFTase and AICARFTase, EC 2.1.2.3, principal mechanism of action, overview. 8, with a 4-carbon bridge, is the most active analog and potently inhibits proliferation of folate receptor alpha-expressing Chinese hamster ovary and KB human tumor cells. Molecular modeling and docking studies, overview
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additional information
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synthesis of 5-substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitors that acts as a dual inhibitor of GARFTase and AICARFTase, EC 2.1.2.3, principal mechanism of action, overview. 8, with a 4-carbon bridge, is the most active analog and potently inhibits proliferation of folate receptor alpha-expressing Chinese hamster ovary and KB human tumor cells. Molecular modeling and docking studies, overview
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additional information
design and synthesis of series of 6-substituted straight side chain pyrrolo[2,3-d]pyrimidines with varying chain lengths (n = 5-8), non-benzoyl 6-carbon chain pyrrolo[2,3-d]pyrimidine antifolates are inhibitors of cell proliferation, correlating with expression of folate receptors. The compounds show selective cellular uptake via folate receptor-alpha and -beta, associated with high affinity binding and inhibition of de novo purine nucleotide biosynthesis via the enzyme, resulting in potent inhibition against folate receptor-expressing Chinese hamster cells and human KB tumor cells in culture
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additional information
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design and synthesis of series of 6-substituted straight side chain pyrrolo[2,3-d]pyrimidines with varying chain lengths (n = 5-8), non-benzoyl 6-carbon chain pyrrolo[2,3-d]pyrimidine antifolates are inhibitors of cell proliferation, correlating with expression of folate receptors. The compounds show selective cellular uptake via folate receptor-alpha and -beta, associated with high affinity binding and inhibition of de novo purine nucleotide biosynthesis via the enzyme, resulting in potent inhibition against folate receptor-expressing Chinese hamster cells and human KB tumor cells in culture
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additional information
design and synthesis of a series of 5-substituted thiopheneyl pyrrolo[2,3-d]pyrimidines with varying chain lengths (n = 1-6). The compounds show dual inhibition of both glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase, analysis of the unique structure-activity relationship for transport and dual target inhibition, molecular modeling and computational studies using crystal structure of human GARFTase at 1.60 A resolution, PDB ID 4EW2, overview
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additional information
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design and synthesis of a series of 5-substituted thiopheneyl pyrrolo[2,3-d]pyrimidines with varying chain lengths (n = 1-6). The compounds show dual inhibition of both glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase, analysis of the unique structure-activity relationship for transport and dual target inhibition, molecular modeling and computational studies using crystal structure of human GARFTase at 1.60 A resolution, PDB ID 4EW2, overview
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