Compounds > ag 2034
Page last updated: 2024-10-15

ag 2034

Description

AG 2034: inhibits glycinamide ribonucleotide formyltransferase; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135465775
CHEBI ID176920
MeSH IDM0274225

Synonyms (19)

Synonym
177575-17-6
CHEBI:176920
(2s)-2-[[5-[2-[(6s)-2-amino-4-oxo-3,6,7,8-tetrahydropyrimido[5,4-b][1,4]thiazin-6-yl]ethyl]thiophene-2-carbonyl]amino]pentanedioic acid
ag 2034
l-glutamic acid, n-((5-(2-((6s)-2-amino-4,6,7,8-tetrahydro-4-oxo-1h-pyrimido(5,4-b)(1,4)thiazin-6-yl)ethyl)-2-thienyl)carbonyl)-
l-glutamic acid, n-((5-(2-(2-amino-4,6,7,8-tetrahydro-4-oxo-1h-pyrimido(5,4-b)(1,4)thiazin-6-yl)ethyl)-2-thienyl)carbonyl)-, (s)-
ag-2034
ag-2033
(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-carbonyl]amino]pentanedioic acid
4-(2-(2-amino-4-oxo-4,6,7,8-tetrahydro-3h-pyrimidino(5,4-6)(1,4)thiazin-6-yl)-(s)-ethyl)-2,5-thienoyl-l-glutamic acid
unii-ic32u30905
ic32u30905 ,
ag2034
C21280
n-((5-(2-(2-amino-4,6,7,8-tetrahydro-4-oxo-1h-pyrimido(5,4-6)(1,4)thiazin-6-yl)ethyl)-2-thienyl)carbonyl)-glutamic acid, s-
DTXSID30938963
n-{5-[2-(4-hydroxy-2-imino-2,6,7,8-tetrahydro-1h-pyrimido[5,4-b][1,4]thiazin-6-yl)ethyl]thiophene-2-carbonyl}glutamic acid
cid 177315
AKOS040747775

Pharmacokinetics

ExcerptReference
" In keeping with this, pharmacokinetic analysis revealed evidence of drug accumulation."( Phase I dose-escalation and pharmacokinetic study of a novel folate analogue AG2034.
Bissett, D; Cassidy, J; Collier, M; McLeod, HL; Paradiso, L; Pithavala, Y; Pitsiladis, M; Sheedy, B, 2001)

Compound-Compound Interactions

ExcerptReference
"The goal of the present report is to compare several published methods of analyzing drug-drug interaction data."( Comparison of methods for evaluating drug-drug interaction.
Au, JL; Wientjes, MG; Zhao, L, 2010)
"The design and analysis of drug combination studies continue to be an area requiring further methodological developments."( Efficient experimental design and nonparametric modeling of drug interaction.
Fang, HB; Tan, M; Yu, T, 2010)

Dosage Studied

ExcerptReference
" "Strong nonlinear blending" is a novel concept that provides a flexible paradigm for the assessment of combination drug synergy that is applicable to any shaped combination-drug dose-response surface; issues of varying relative potency, partial inhibitors, potentiation, or coalism pose no problems at all."( A review of synergy concepts of nonlinear blending and dose-reduction profiles.
Peterson, JJ, 2010)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
glutamic acid derivativeAn amino acid derivative resulting from reaction of glutamic acid at the amino group or either of the carboxy groups, or from the replacement of any hydrogen by a heteroatom. The definition normally excludes peptides containing glutamic acid residues.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (26.32)18.2507
2000's7 (36.84)29.6817
2010's7 (36.84)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (15.79%)5.53%
Reviews1 (5.26%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (78.95%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
purine
1H-purine : The 1H-tautomer of purine.. 3H-purine : The 3H-tautomer of purine.. 9H-purine : The 9H-tautomer of purine.. 7H-purine : The 7H-tautomer of purine.		2.4220purine
pyrimethamine
Maloprim: contains above 2 cpds		1.9910aminopyrimidine;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
trimetrexate
Trimetrexate: A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect.		4.92110
thymidine
[no description available]		2.0110pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
metabolite;
mouse metabolite
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		2.0110mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		2.0110azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
methotrexate
[no description available]		2.420dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
hypoxanthine
[no description available]		2.7230nucleobase analogue;
oxopurine;
purine nucleobase		fundamental metabolite
folic acid
folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin.		4.83100folic acids;
N-acyl-amino acid		human metabolite;
mouse metabolite;
nutrient
raltitrexed
[no description available]		2.0110N-acyl-amino acid
lometrexol
lometrexol: RN & structure given in first source;		2.4120
ConditionIndicatedRelationship StrengthStudiesTrials
Adenocarcinoma, Basal Cell
[description not available]		02.7130
Cancer of Prostate
[description not available]		02.4520
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		02.7130
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		02.4520
Cancer of Colon
[description not available]		02.4120
Leukemia L 1210
[description not available]		02.0110
Benign Neoplasms
[description not available]		05.2243
Colonic Neoplasms
Tumors or cancer of the COLON.		02.4120
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		05.2243
Cancer of ILEUM
[description not available]		02.0110
Cancer of Cecum
[description not available]		02.0110
Experimental Neoplasms
[description not available]		01.9910
Leucocythaemia
[description not available]		01.9910
Leukemia
A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006)		01.9910
Carcinoma, Epidermoid
[description not available]		0210
Cancer of Head
[description not available]		0210
Cancer of Lung
[description not available]		0210
Carcinoma, Squamous Cell
A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)		0210
Head and Neck Neoplasms
Soft tissue tumors or cancer arising from the mucosal surfaces of the LIP; oral cavity; PHARYNX; LARYNX; and cervical esophagus. Other sites included are the NOSE and PARANASAL SINUSES; SALIVARY GLANDS; THYROID GLAND and PARATHYROID GLANDS; and MELANOMA and non-melanoma skin cancers of the head and neck. (from Holland et al., Cancer Medicine, 4th ed, p1651)		0210
Lung Neoplasms
Tumors or cancer of the LUNG.		0210
Mucositis, Oral
[description not available]		03.3911
Thrombopenia
[description not available]		03.3911
Diarrhea
An increased liquidity or decreased consistency of FECES, such as running stool. Fecal consistency is related to the ratio of water-holding capacity of insoluble solids to total water, rather than the amount of water present. Diarrhea is not hyperdefecation or increased fecal weight.		03.3911
Nausea
An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.		03.3911
Neutropenia
A decrease in the number of NEUTROPHILS found in the blood.		03.3911
Stomatitis
INFLAMMATION of the soft tissues of the MOUTH, such as MUCOSA; PALATE; GINGIVA; and LIP.		03.3911
Thrombocytopenia
A subnormal level of BLOOD PLATELETS.		03.3911