Compounds > eapb0503
Page last updated: 2024-11-13

eapb0503

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

Description

EAPB0503: antineoplastic; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID25253256
CHEMBL ID557421
SCHEMBL ID2817762
MeSH IDM0554698

Synonyms (10)

Synonym
CHEMBL557421
SCHEMBL2817762
eapb 0503
eapb0503
unii-y8us5i7e55
1140627-77-5
imidazo(1,2-a)quinoxalin-4-amine, 1-(3-methoxyphenyl)-n-methyl-
eapb-0503
y8us5i7e55 ,
1-(3-methoxyphenyl)-n-methylimidazo(1,2-a)quinoxalin-4-amine

Research Excerpts

Effects

ExcerptReferenceRelevance
"EAPB0503 has been shown to inhibit tubulin polymerization."( Imidazoquinoxaline anticancer derivatives and imiquimod interact with tubulin: Characterization of molecular microtubule inhibiting mechanisms in correlation with cytotoxicity.
Bec, N; Constant, C; Courbet, A; Deleuze-Masquefa, C; El Messaoudi, S; Gattacceca, F; Khier, S; Larroque, C; Pugniere, M; Zghaib, Z, 2017)		1.18

Pharmacokinetics

ExcerptReferenceRelevance
" This method was successfully implemented to support a mouse pharmacokinetic study following a single intraperitoneal administration of EAPB02303 in male C57Bl/6 mice."( Liquid chromatography-electrospray ionization-tandem mass spectrometry method for quantitative estimation of new imiqualine leads with potent anticancer activities in rat and mouse plasma. Application to a pharmacokinetic study in mice.
Bonnet, PA; Bressolle-Gomeni, FMM; Chouchou, A; Cuq, P; Deleuze-Masquéfa, C; Enjalbal, C; Marion, B; Roques, C, 2018)		0.48

Bioavailability

ExcerptReferenceRelevance
" After intraperitoneal administration, bioavailability was 22."( Metabolism and pharmacokinetics of EAPB0203 and EAPB0503, two imidazoquinoxaline compounds previously shown to have antitumoral activity on melanoma and T-lymphomas.
Bompart, J; Bonnet, PA; Bressolle, FM; Cooper, JF; Deleuze-Masquéfa, C; El Messaoudi, S; Gattacceca, F; Khier, S; Lafaille, F; Pinguet, F; Solassol, I, 2010)		0.62

Dosage Studied

ExcerptRelevanceReference
" The obtained pharmacokinetic parameters of EAPB02303 would be useful to optimize the dosing and the rhythm of administration for subsequent preclinical in vivo activity studies."( Liquid chromatography-electrospray ionization-tandem mass spectrometry method for quantitative estimation of new imiqualine leads with potent anticancer activities in rat and mouse plasma. Application to a pharmacokinetic study in mice.
Bonnet, PA; Bressolle-Gomeni, FMM; Chouchou, A; Cuq, P; Deleuze-Masquéfa, C; Enjalbal, C; Marion, B; Roques, C, 2018)		0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID1729588Antiproliferative activity against human IPC-298 cells assessed as reduction in cell viability measured after 96 hrs by MTT assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Imidazo[1,2-a]quinoxalines for melanoma treatment with original mechanism of action.
AID1292221Inhibition of human recombinant His tagged IKK1 expressed in baculovirus at 10 uM after 60 mins by Adapta assay2016European journal of medicinal chemistry, Jun-10, Volume: 115New IKK inhibitors: Synthesis of new imidazo[1,2-a]quinoxaline derivatives using microwave assistance and biological evaluation as IKK inhibitors.
AID1729585Antiproliferative activity against human A-375 cells assessed as reduction in cell viability measured after 96 hrs by MTT assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Imidazo[1,2-a]quinoxalines for melanoma treatment with original mechanism of action.
AID1729586Antiproliferative activity against human MeWo cells assessed as reduction in cell viability measured after 96 hrs by MTT assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Imidazo[1,2-a]quinoxalines for melanoma treatment with original mechanism of action.
AID433907Cytotoxicity against human A375 cells after 96 hrs by MTT assay2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
New imidazo[1,2-a]quinoxaline derivatives: synthesis and in vitro activity against human melanoma.
AID1729587Antiproliferative activity against human A2058 cells assessed as reduction in cell viability measured after 96 hrs by MTT assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Imidazo[1,2-a]quinoxalines for melanoma treatment with original mechanism of action.
AID1292355Inhibition of pig brain tubulin polymerization at 5 uM by spectrophotometric analysis2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
New imidazoquinoxaline derivatives: Synthesis, biological evaluation on melanoma, effect on tubulin polymerization and structure-activity relationships.
AID1292357Cell cycle arrest in human A375 cells assessed as effect on number of cells at S phase after 24 hrs by propidium iodide staining based flow cytometric analysis2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
New imidazoquinoxaline derivatives: Synthesis, biological evaluation on melanoma, effect on tubulin polymerization and structure-activity relationships.
AID1729584Inhibition of pig brain tubulin polymerization at 5 uM measured after 45 mins by turbidimetry based spectrophotometric method relative to control2021European journal of medicinal chemistry, Feb-15, Volume: 212Imidazo[1,2-a]quinoxalines for melanoma treatment with original mechanism of action.
AID1292354Antiproliferative activity against human A375 cells assessed as cell growth inhibition after 96 hrs by MTT assay2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
New imidazoquinoxaline derivatives: Synthesis, biological evaluation on melanoma, effect on tubulin polymerization and structure-activity relationships.
AID1292222Inhibition of human recombinant GST tagged IKK2 expressed in baculovirus using Ser/Thr05 peptide as substrate at 10 uM after 60 mins by Z-LYTE assay2016European journal of medicinal chemistry, Jun-10, Volume: 115New IKK inhibitors: Synthesis of new imidazo[1,2-a]quinoxaline derivatives using microwave assistance and biological evaluation as IKK inhibitors.
AID1292356Cell cycle arrest in human A375 cells assessed as effect on number of cells at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometric analysis2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
New imidazoquinoxaline derivatives: Synthesis, biological evaluation on melanoma, effect on tubulin polymerization and structure-activity relationships.
AID1292358Cell cycle arrest in human A375 cells assessed as accumulation of cells at G2/M phase after 24 hrs by propidium iodide staining based flow cytometric analysis2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
New imidazoquinoxaline derivatives: Synthesis, biological evaluation on melanoma, effect on tubulin polymerization and structure-activity relationships.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (8.33)29.6817
2010's9 (75.00)24.3611
2020's2 (16.67)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 (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
colchicine
(S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.		2.8730alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
quinoxalines
quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.		3.6480mancude organic heterobicyclic parent;
naphthyridine;
ortho-fused heteroarene
imiquimod
Imiquimod: A topically-applied aminoquinoline immune modulator that induces interferon production. It is used in the treatment of external genital and perianal warts, superficial CARCINOMA, BASAL CELL; and ACTINIC KERATOSIS.. imiquimod : An imidazoquinoline fused [4,5-c] carrying isobutyl and amino substituents at N-1 and C-4 respectively. A prescription medication, it acts as an immune response modifier and is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis.		7.4920imidazoquinolineantineoplastic agent;
interferon inducer
fotemustine
fotemustine: structure given in first source. fotemustine : A racemate comprising equimolar amounts of (R)- and (S)-fotemustine. It is an alkylating agent used in the treatment of malignant melanoma.. diethyl (1-{[(2-chloroethyl)(nitroso)carbamoyl]amino}ethyl)phosphonate : A member of the class of N-nitrosoureas that is ethyl diethylphosphonate in the hydrogen at position 1 of the ethyl group attached to the phosphorus has been replaced by a [(2-chloroethyl)(nitroso)carbamoyl]amino group.		2.0510N-nitrosoureas;
organic phosphonate;
organochlorine compound
imatinib mesylate
imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.		2.110methanesulfonate saltanticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
bms345541
[no description available]		2.1310
eapb0203
EAPB0203: antineoplastic; structure in first source		8.1950
ConditionIndicatedRelationship StrengthStudiesTrials
Malignant Melanoma
[description not available]		02.7630
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		07.7630
B16 Melanoma
[description not available]		02.3110
Acute Myelogenous Leukemia
[description not available]		02.6320
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		02.6320
Leishmaniasis, American
[description not available]		02.1710
Leishmaniasis, Cutaneous
An endemic disease that is characterized by the development of single or multiple localized lesions on exposed areas of skin that typically ulcerate. The disease has been divided into Old and New World forms. Old World leishmaniasis is separated into three distinct types according to epidemiology and clinical manifestations and is caused by species of the L. tropica and L. aethiopica complexes as well as by species of the L. major genus. New World leishmaniasis, also called American leishmaniasis, occurs in South and Central America and is caused by species of the L. mexicana or L. braziliensis complexes.		02.1710
Granulocytic Leukemia, Chronic
[description not available]		02.110
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Clonal hematopoetic disorder caused by an acquired genetic defect in PLURIPOTENT STEM CELLS. It starts in MYELOID CELLS of the bone marrow, invades the blood and then other organs. The condition progresses from a stable, more indolent, chronic phase (LEUKEMIA, MYELOID, CHRONIC PHASE) lasting up to 7 years, to an advanced phase composed of an accelerated phase (LEUKEMIA, MYELOID, ACCELERATED PHASE) and BLAST CRISIS.		02.110
T-Cell Lymphoma
[description not available]		02.0510
Lymphoma, T-Cell
A group of heterogeneous lymphoid tumors representing malignant transformations of T-lymphocytes.		02.0510