Page last updated: 2024-12-06

methasquin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

methasquin: folic acid antagonist that has been used in the treatment of experimental leukemia; acts by inhibiting the dihydrofolate reductase in the cell; minor descriptor (75-85); on-line & Index Medicus search ASPARTIC ACID/AA (75-85); RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	29335
CHEMBL ID	154418
MeSH ID	M0262979

Synonyms (7)

Synonym
aspartic acid,4-diamino-5-methyl-6-quinazolinyl)methyl]amino] benzoyl]-, l-
l-aspartic acid,4-diamino-5-methyl-6-quinazolinyl)methyl]amino] benzoyl]-,
methasquin
2-[[4-[(2,4-diamino-5-methyl-quinazolin-6-yl)methylamino]benzoyl]amino]butanedioic acid
nsc122870
l-aspartic acid, n-[4-[[(2,4-diamino-5-methyl-6-quinazolinyl)methyl]-
CHEMBL154418

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (7)

Assay ID	Title	Year	Journal	Article
AID1123092	Inhibition of thymidylate synthetase in Lactobacillus casei	1979	Journal of medicinal chemistry, May, Volume: 22, Issue:5	Multivariate analysis and quantitative structure-activity relationships. Inhibition of dihydrofolate reductase and thymidylate synthetase by quinazolines.
AID1123091	Inhibition of thymidylate synthetase in mouse L1210S cells	1979	Journal of medicinal chemistry, May, Volume: 22, Issue:5	Multivariate analysis and quantitative structure-activity relationships. Inhibition of dihydrofolate reductase and thymidylate synthetase by quinazolines.
AID1123094	Inhibition of dihydrofolate reductase in mouse L1210R cells	1979	Journal of medicinal chemistry, May, Volume: 22, Issue:5	Multivariate analysis and quantitative structure-activity relationships. Inhibition of dihydrofolate reductase and thymidylate synthetase by quinazolines.
AID56152	Binding energy against Streptococcus faecium dihydrofolate reductase	1980	Journal of medicinal chemistry, Jun, Volume: 23, Issue:6	Quantitative structure-activity relationships by distance geometry: systematic analysis of dihydrofolate reductase inhibitors.
AID1146760	Inhibition of Streptococcus faecium dihydrofolate reductase using dihydrofolate as substrate	1977	Journal of medicinal chemistry, Jan, Volume: 20, Issue:1	Quantitative structure-activity relationships of antimalarial and dihydrofolate reductase inhibition by quinazolines and 5-substituted benzyl-2,4-diaminopyrimidines.
AID56148	Binding energy to Streptococcus faecium dihydrofolate reductase	1982	Journal of medicinal chemistry, Aug, Volume: 25, Issue:8	Quantitative structure-activity relationship by distance geometry: quinazolines as dihydrofolate reductase inhibitors.
AID1123093	Inhibition of dihydrofolate reductase in human acute lymphocytic leukemia cells	1979	Journal of medicinal chemistry, May, Volume: 22, Issue:5	Multivariate analysis and quantitative structure-activity relationships. Inhibition of dihydrofolate reductase and thymidylate synthetase by quinazolines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	6 (100.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	0 (0.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	1 (14.29%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	6 (85.71%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
pyrimethamine Maloprim: contains above 2 cpds	1.96	1	aminopyrimidine; monochlorobenzenes	antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor
trimethoprim Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge.	1.95	1	aminopyrimidine; methoxybenzenes	antibacterial drug; diuretic; drug allergen; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; environmental contaminant; xenobiotic
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.	1.95	1
aspartic acid Aspartic Acid: One of the non-essential amino acids commonly occurring in the L-form. It is found in animals and plants, especially in sugar cane and sugar beets. It may be a neurotransmitter.. aspartic acid : An alpha-amino acid that consists of succinic acid bearing a single alpha-amino substituent. L-aspartic acid : The L-enantiomer of aspartic acid.	2.36	2	aspartate family amino acid; aspartic acid; L-alpha-amino acid; proteinogenic amino acid	Escherichia coli metabolite; mouse metabolite; neurotransmitter
adamantane Adamantane: A tricyclo bridged hydrocarbon.	1.96	1	adamantanes; polycyclic alkane
diaveridine diaveridine: RN given refers to parent cpd; structure. diaveridine : An aminopyrimidine in which the pyrimidine ring carries amino substituents at C-2 and C-4 and a 3,4-dimethoxybenzyl group at C-5. A folic acid antagonist, it is used as a synergist with sulfonamides against the parasitic Eimeria species.	1.95	1	aminopyrimidine	antiparasitic agent; drug allergen
metoprine metoprine: histamine methyltransferase antagonist	1.96	1
piritrexim piritrexim: RN given refers to parent cpd; structure given in first source	1.96	1
2,4-diamino-5-adamantyl-6-methylpyrimidine [no description available]	1.96	1
2,4-diamino-5-benzylpyrimidine 2,4-diamino-5-benzylpyrimidine: structure given in first source	1.95	1
pam 1392 [no description available]	1.95	1
wr 158122 WR 158122: structure	2.65	3
cb 3703 CB 3703: inhibitor of dihydrofolate reductase & thymidylate synthetase; RN given refers to parent cpd	1.95	1
wr 159412 [no description available]	2.65	3
methotrexate [no description available]	7.36	2	dicarboxylic 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
nitroquine nitroquine: RN given refers to parent cpd	1.95	1
(5)n,(8)n-deaza-(10)-n-methylfolate [no description available]	2.87	4

Condition	Relationship Strength	Studies
Leukemia L 1210 [description not available]	1.95	1
Leukemia, Lymphocytic [description not available]	1.95	1
Leukemia, Lymphoid Leukemia associated with HYPERPLASIA of the lymphoid tissues and increased numbers of circulating malignant LYMPHOCYTES and lymphoblasts.	1.95	1

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