Page last updated: 2024-12-08
agelastatin a
Description
Research Excerpts
Clinical Trials
Roles
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Pathways
Study Profile
Bioassays
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Market Indicators
Description
agelastatin A: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 177936 |
CHEMBL ID | 1096256 |
SCHEMBL ID | 4745999 |
MeSH ID | M0438264 |
Synonyms (17)
Synonym |
---|
(-)-agelastatin a |
CHEMBL1096256 |
agelastatin a |
agelastatine a |
152406-28-5 |
imidazo(4',5':4,5)cyclopenta(1,2-e)pyrrolo(1,2-a)pyrazine-4,7-dione, 1-bromo-5,5a,5b,6,8,8a,9,9a-octahydro-8a-hydroxy-8-methyl-, (5as-(5aalpha,5bbeta,8abeta,9aalpha))- |
SCHEMBL4745999 |
MPASKXAEPUAMBS-WJOUQXRDSA-N |
7MB , |
DTXSID60934493 |
1-bromo-7,8a-dihydroxy-8-methyl-5a,5b,8,8a,9,9a-hexahydroimidazo[4',5':4,5]cyclopenta[1,2-e]pyrrolo[1,2-a]pyrazin-4(5h)-one |
(1r,9s,10s,14s)-3-bromo-14-hydroxy-13-methyl-2,8,11,13-tetrazatetracyclo[7.6.0.02,6.010,14]pentadeca-3,5-diene-7,12-dione |
nsc-786147 |
nsc786147 |
HY-125132 |
CS-0089439 |
AKOS040747602 |
Research Excerpts
Overview
Agelastatin A is a naturally occurring oroidin alkaloid with powerful antitumor effects that, in many cases, are superior to cisplatin in vitro.
Excerpt | Reference | Relevance |
---|---|---|
"Agelastatin A is a marine alkaloid with potent biological activity. " | ( The D'Ambrosio, M, 2023) | 2.35 |
"(-)-Agelastatin A is a naturally occurring oroidin alkaloid with powerful antitumor effects that, in many cases, are superior to cisplatin in vitro." | ( Agelastatin A: a novel inhibitor of osteopontin-mediated adhesion, invasion, and colony formation. Campbell, FC; Crowe, P; Domostoj, MM; El-Tanani, M; Erwin, PJ; Hale, KJ; Johnston, PG; Manaviazar, S; Mason, CK; McFarlane, S, 2008) | 2.27 |
Treatment
Excerpt | Reference | Relevance |
---|---|---|
"(-)-Agelastatin A treatment also reduced beta-catenin protein expression and reduced anchorage-independent growth, adhesion, and invasion in R37 OPN pBK-CMV and C9 cell lines." | ( Agelastatin A: a novel inhibitor of osteopontin-mediated adhesion, invasion, and colony formation. Campbell, FC; Crowe, P; Domostoj, MM; El-Tanani, M; Erwin, PJ; Hale, KJ; Johnston, PG; Manaviazar, S; Mason, CK; McFarlane, S, 2008) | 2.27 |
Pharmacokinetics
Excerpt | Reference | Relevance |
---|---|---|
" A detailed in vitro structure-activity relationship of 1a in CLL compared to that of 22 synthetic analogues is described along with preliminary in vivo pharmacokinetic and metabolism studies on the most potent compounds." | ( Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. Castro, JE; Choi, MY; Molinski, TF; Stout, EP, 2014) | 0.73 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Bioassays (50)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1223770 | Solubility of compound in water at 25 degC | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223775 | Half life in BALB/c mouse plasma at 2.5 mg/kg, iv administered as single dose by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223795 | Drug recovery in BALB/c mouse serum at 50 uM after 24 hrs by LC-MS method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223792 | Protein binding in BALB/c mouse serum at 50 uM after 1 to 24 hrs by LC-MS method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223781 | Cmax in BALB/c mouse plasma at 5 mg/kg, ip administered as single dose by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223774 | Tmax in BALB/c mouse plasma at 2.5 mg/kg, iv administered as single dose by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223762 | Antitumor activity against CLL1 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1290975 | Cytotoxicity against human OVACR3 cells after 48 hrs by crystal violet staining based assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID1223786 | Metabolic stability in mouse liver microsomes containing glucuronidase | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223796 | Drug recovery in human AB serum at 50 uM after 24 hrs by LC-MS method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223782 | Tmax in BALB/c mouse plasma at 5 mg/kg, ip administered as single dose by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1290978 | Plasma protein binding in human by liquid chromatography-mass spectrometric analysis | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID1223780 | AUC in BALB/c mouse plasma at 5 mg/kg, ip administered as single dose by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223765 | Antitumor activity against human HeLa cells assessed as cell viability by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223768 | Antitumor activity against CLL5 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223779 | Half life in BALB/c mouse plasma at 2.5 mg/kg, ip administered as single dose by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID477229 | Cytotoxicity against human KB cells at 30 uM | 2010 | Journal of natural products, Apr-23, Volume: 73, Issue:4 | Agelastatin E, agelastatin F, and benzosceptrin C from the marine sponge Agelas dendromorpha. |
AID1290973 | Cytotoxicity against human A3 cells after 48 hrs by crystal violet staining based assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID1223776 | AUC in BALB/c mouse plasma at 2.5 mg/kg, ip administered as single dose by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223764 | Antitumor activity against human JVM2 cells assessed as cell viability after 48 hrs by FACS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223777 | Cmax in BALB/c mouse plasma at 2.5 mg/kg, ip administered as single dose by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1290979 | Metabolic stability in human plasma assessed as drug recovery | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID1223773 | Cmax in BALB/c mouse plasma at 2.5 mg/kg, iv administered as single dose by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1290982 | Cytotoxicity against human B cells assessed as cell viability after 24 hrs by annexin V/propidium iodide staining based flow cytometric analysis | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID1290969 | Cytotoxicity against human HeLa cells after 24 hrs by [3H]-thymidine incorporation assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID1223788 | Drug excretion in BALB/c mouse urine at 2.5 mg/kg, ip administered as single dose measured after 5 mins by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223794 | Drug recovery in BALB/c mouse plasma at 50 uM after 24 hrs by LC-MS method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223784 | Metabolic stability in human liver microsomes at 100 uM measured after 1 hr by LC/MS analysis in presence of 1 mM NADPH | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223793 | Protein binding in human AB serum at 50 uM after 1 to 24 hrs by LC-MS method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223778 | Tmax in BALB/c mouse plasma at 2.5 mg/kg, ip administered as single dose by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1290972 | Cytotoxicity against human SJSA1 cells after 48 hrs by crystal violet staining based assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID1223772 | AUC in BALB/c mouse plasma at 2.5 mg/kg, iv administered as single dose by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223763 | Antitumor activity against CLL2 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1290971 | Cytotoxicity against human CLL cells after 24 hrs by annexin-V/PI staining based flow cytometry | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID1223785 | Metabolic stability in mouse liver microsomes at 100 uM measured after 1 hr by LC/MS analysis in presence of 1 mM NADPH | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1290970 | Cytotoxicity against human IGROV cells after 48 hrs by crystal violet staining based assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID1223783 | Half life in BALB/c mouse plasma at 5 mg/kg, ip administered as single dose by LC/MS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1290974 | Cytotoxicity against human A431 cells after 48 hrs by crystal violet staining based assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID477228 | Cytotoxicity against human KB cells at 3 uM | 2010 | Journal of natural products, Apr-23, Volume: 73, Issue:4 | Agelastatin E, agelastatin F, and benzosceptrin C from the marine sponge Agelas dendromorpha. |
AID1223790 | Cytotoxicity against human CLL cells | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1290976 | Cytotoxicity against human CLL cells after 24 hrs by annexin-V/PI staining based flow cytometry in presence of human plasma protein | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID1223766 | Antitumor activity against CLL3 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1290977 | Cytotoxicity against human CLL cells after 24 hrs by annexin-V/PI staining based flow cytometry in presence of fetal bovine serum | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID1223769 | Antitumor activity against CLL6 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223767 | Antitumor activity against CLL4 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223789 | Cytotoxicity against human KB cells | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1290983 | Cytotoxicity against human T cells assessed as cell viability after 24 hrs by annexin V/propidium iodide staining based flow cytometric analysis | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe. |
AID1223771 | Lipophilicity, log P of compound at 25 degC | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223787 | Metabolic stability in human liver S9 fraction containing glucuronidase | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
AID1223791 | Protein binding in BALB/c mouse plasma at 50 uM after 1 to 24 hrs by LC-MS method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (29)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 15 (51.72) | 29.6817 |
2010's | 12 (41.38) | 24.3611 |
2020's | 2 (6.90) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 22.73
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (22.73) All Compounds (24.57) |
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 | 29 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |