Compounds > eapb0203

Page last updated: 2024-11-13

eapb0203

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

Description

EAPB0203: antineoplastic; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	24779760
CHEMBL ID	488644
SCHEMBL ID	2815787
MeSH ID	M0521340

Synonyms (10)

Synonym
CHEMBL488644
SCHEMBL2815787
eapb-0203
eapb0203
kxz9la2qv7 ,
imidazo(1,2-a)quinoxalin-4-amine, n-methyl-1-(2-phenylethyl)-
unii-kxz9la2qv7
eapb 0203
681284-86-6
n-methyl-1-(2-phenylethyl)imidazo(1,2-a)quinoxalin-4-amine

Research Excerpts

Treatment

Excerpt	Reference	Relevance
"EAPB0203 treatment significantly down-regulated the antiapoptotic proteins c-IAP-1 and Bcl-XL and resulted in a significant loss of mitochondrial membrane potential, cytoplasmic release of cytochrome c, and caspase-dependent apoptosis."	( EAPB0203, a member of the imidazoquinoxaline family, inhibits growth and induces caspase-dependent apoptosis in T-cell lymphomas and HTLV-I-associated adult T-cell leukemia/lymphoma. Bazarbachi, A; Bonnet, PA; Deleuze-Masquéfa, C; El-Hajj, H; El-Sabban, ME; Hermine, O; Kfoury, Y; Lepelletier, Y; Moarbess, G, 2008)	2.51

Pharmacokinetics

Excerpt	Reference	Relevance
" 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

Excerpt	Reference	Relevance
" After intraperitoneal administration the absolute bioavailability remains limited (22."	( Pharmacology of EAPB0203, a novel imidazo[1,2-a]quinoxaline derivative with anti-tumoral activity on melanoma. Bonnet, PA; Bressolle, FM; Cooper, JF; Deleuze-Masquéfa, C; Gattacceca, F; Khier, S; Margout, D; Moarbess, G; Pinguet, F; Solassol, I, 2010)	0.71
" 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)	0.64

Dosage Studied

Excerpt	Relevance	Reference
" 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 (9)

Assay ID	Title	Year	Journal	Article
AID406724	Cytotoxicity against human M4Be cells after 96 hrs by MTT assay	2008	Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13	In vitro and in vivo anti-tumoral activities of imidazo[1,2-a]quinoxaline, imidazo[1,5-a]quinoxaline, and pyrazolo[1,5-a]quinoxaline derivatives.
AID406729	Antitumor activity against human M4Be cells xenografted Swiss nude mouse assessed as reduction in tumor volume at 20 mg/kg, ip administered twice a week for 3 weeks measured from day 18 to day 55	2008	Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13	In vitro and in vivo anti-tumoral activities of imidazo[1,2-a]quinoxaline, imidazo[1,5-a]quinoxaline, and pyrazolo[1,5-a]quinoxaline derivatives.
AID433907	Cytotoxicity against human A375 cells after 96 hrs by MTT assay	2009	European journal of medicinal chemistry, Sep, Volume: 44, Issue:9	New imidazo[1,2-a]quinoxaline derivatives: synthesis and in vitro activity against human melanoma.
AID406726	Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay	2008	Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13	In vitro and in vivo anti-tumoral activities of imidazo[1,2-a]quinoxaline, imidazo[1,5-a]quinoxaline, and pyrazolo[1,5-a]quinoxaline derivatives.
AID406728	Cytotoxicity against human Raji cells after 96 hrs by MTT assay	2008	Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13	In vitro and in vivo anti-tumoral activities of imidazo[1,2-a]quinoxaline, imidazo[1,5-a]quinoxaline, and pyrazolo[1,5-a]quinoxaline derivatives.
AID406725	Cytotoxicity against human RPMI7591 cells after 96 hrs by MTT assay	2008	Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13	In vitro and in vivo anti-tumoral activities of imidazo[1,2-a]quinoxaline, imidazo[1,5-a]quinoxaline, and pyrazolo[1,5-a]quinoxaline derivatives.
AID406730	Toxicity in ip dosed Swiss mouse	2008	Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13	In vitro and in vivo anti-tumoral activities of imidazo[1,2-a]quinoxaline, imidazo[1,5-a]quinoxaline, and pyrazolo[1,5-a]quinoxaline derivatives.
AID406727	Cytotoxicity against human LS174T cells after 96 hrs by MTT assay	2008	Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13	In vitro and in vivo anti-tumoral activities of imidazo[1,2-a]quinoxaline, imidazo[1,5-a]quinoxaline, and pyrazolo[1,5-a]quinoxaline derivatives.
AID406723	Cytotoxicity against human A375 cells after 96 hrs by MTT assay	2008	Bioorganic & medicinal chemistry, Jul-01, Volume: 16, Issue:13	In vitro and in vivo anti-tumoral activities of imidazo[1,2-a]quinoxaline, imidazo[1,5-a]quinoxaline, and pyrazolo[1,5-a]quinoxaline derivatives.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	3 (33.33)	29.6817
2010's	6 (66.67)	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	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	9 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
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.	2.15	1	0	alkaloid; colchicine	anti-inflammatory agent; gout suppressant; mutagen
quinoxalines quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.	3.47	7	0	mancude 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.	2.96	4	0	imidazoquinoline	antineoplastic agent; interferon inducer
irinotecan [no description available]	2.04	1	0	carbamate ester; delta-lactone; N-acylpiperidine; pyranoindolizinoquinoline; ring assembly; tertiary alcohol; tertiary amino compound	antineoplastic agent; apoptosis inducer; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug
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.	2.74	3	0	N-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.	2.1	1	0	methanesulfonate salt	anticoronaviral agent; antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor
methotrexate [no description available]	2.04	1	0	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
cytochrome c-t Cytochromes c: Cytochromes of the c type that are found in eukaryotic MITOCHONDRIA. They serve as redox intermediates that accept electrons from MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX III and transfer them to MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX IV.	2.04	1	0
eapb0503 EAPB0503: antineoplastic; structure in first source	8.19	5	0

Condition	Indicated	Relationship Strength	Studies	Trials
Malignant Melanoma [description not available]	0	2.74	3	0
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)	0	2.74	3	0
Granulocytic Leukemia, Chronic [description not available]	0	2.1	1	0
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.	0	2.1	1	0
Cancer of Skin [description not available]	0	2.45	2	0
Skin Neoplasms Tumors or cancer of the SKIN.	0	2.45	2	0
T-Cell Lymphoma [description not available]	0	7.45	2	0
Lymphoma, T-Cell A group of heterogeneous lymphoid tumors representing malignant transformations of T-lymphocytes.	0	2.45	2	0
Innate Inflammatory Response [description not available]	0	2.04	1	0
ATLL [description not available]	0	2.04	1	0
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	2.04	1	0
Leukemia-Lymphoma, Adult T-Cell Aggressive T-Cell malignancy with adult onset, caused by HUMAN T-LYMPHOTROPIC VIRUS 1. It is endemic in Japan, the Caribbean basin, Southeastern United States, Hawaii, and parts of Central and South America and sub-Saharan Africa.	0	2.04	1	0