Compounds > deacetoxyvinzolidine
Page last updated: 2024-12-08

deacetoxyvinzolidine

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

Description

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

Cross-References

ID SourceID
PubMed CID157684
MeSH IDM0280382

Synonyms (15)

Synonym
kar-2
1XA5 ,
DB02868
deacetoxyvinzolidine
3''-(beta-chloroethyl)-2'',4''-dioxo-3,5''-spirooxazolidino-4-deacetoxyvinblastine
unii-6pbv11io5e
methyl (3r-(3r*,5s*,7r*,9s*))-9-((2beta,3beta,5alpha,12beta,19alpha)-3'-(2-chloroethyl)-6,7-didehydro-16-methoxy-1-methyl-2',4'-dioxospiro(aspidospermidine-3,5'-oxazolidin)-15-yl)-5-ethyl-1,4,5,6,7,8,9,10-octahydro-5-hydroxy-2h-3,7-methanoazacycloundecino
165659-77-8
6pbv11io5e ,
2h-3,7-methanoazacycloundecino(5,4-b)indole-9-carboxylic acid, 9-((2beta,3beta,5alpha,12beta,19alpha)-3'-(2-chloroethyl)-6,7-didehydro-16-methoxy-1-methyl-2',4'-dioxospiro(aspidospermidine-3,5'-oxazolidin)-15-yl)-5-ethyl-1,4,5,6,7,8,9,10-octahydro-5-hydro
3''-(.beta.-chloroethyl)-3-spiro-2'',4''-dioxo-5-oxazolidino-4'-deacetoxyvinblastine
methyl (5s,7r,9s)-9-[(3ar,5r,5ar,10br,13as)-3'-(2-chloroethyl)-3a-ethyl-8-methoxy-6-methyl-2',4'-dioxo-3a,5a,6,11,12,13a-hexahydro-1h,4h-spiro[indolizino[8,1-cd]carbazole-5,5'-[1,3]oxazolidin]-9-yl]-5-ethyl-5-hydroxy-1,4,5,6,7,8,9,10-octahydro-2h-3,7-meth
Q27265278
methyl (13s,15r,17s)-13-[(1'r,5r,9'r,12'r,19's)-3-(2-chloroethyl)-12'-ethyl-5'-methoxy-8'-methyl-2,4-dioxospiro[1,3-oxazolidine-5,10'-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraene]-4'-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[
AKOS040751427

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Their use in clinical chemotherapy is still limited because of: (i) the non-specific targeting of the mitotic cells; (ii) low bioavailability of the drugs."( Unique pharmacology of KAR-2, a potential anti-cancer agent: absorption modelling and selective mitotic spindle targeting.
Bermejo, M; Gonzalez-Alvarez, I; Gonzalez-Alvarez, M; Merino, V; Oltra-Noguera, D; Ovádi, J; Tõkési, N, 2009)		0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, CalmodulinBos taurus (cattle)Kd0.31600.31600.31600.3160AID977611
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2005The Journal of biological chemistry, Mar-04, Volume: 280, Issue:9
The structure of the complex of calmodulin with KAR-2: a novel mode of binding explains the unique pharmacology of the drug.
AID1811Experimentally measured binding affinity data derived from PDB2005The Journal of biological chemistry, Mar-04, Volume: 280, Issue:9
The structure of the complex of calmodulin with KAR-2: a novel mode of binding explains the unique pharmacology of the drug.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (40.00)18.2507
2000's5 (50.00)29.6817
2010's1 (10.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.86

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.86 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.86)

All Compounds (24.57)

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%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
trifluoperazine
[no description available]		2.6930N-alkylpiperazine;
N-methylpiperazine;
organofluorine compound;
phenothiazines		antiemetic;
calmodulin antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor;
phenothiazine antipsychotic drug
thapsigargin
Thapsigargin: A sesquiterpene lactone found in roots of THAPSIA. It inhibits SARCOPLASMIC RETICULUM CALCIUM-TRANSPORTING ATPASES.. thapsigargin : An organic heterotricyclic compound that is a hexa-oxygenated 6,7-guaianolide isolated fron the roots of Thapsia garganica L., Apiaceae. A potent skin irritant, it is used in traditional medicine as a counter-irritant. Thapsigargin inhibits Ca(2+)-transporting ATPase mediated uptake of calcium ions into sarcoplasmic reticulum and is used in experimentation examining the impacts of increasing cytosolic calcium concentrations.		210butyrate ester;
organic heterotricyclic compound;
sesquiterpene lactone		calcium channel blocker;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor
melitten
Melitten: Basic polypeptide from the venom of the honey bee (Apis mellifera). It contains 26 amino acids, has cytolytic properties, causes contracture of muscle, releases histamine, and disrupts surface tension, probably due to lysis of cell and mitochondrial membranes.		1.9910
ConditionIndicatedRelationship StrengthStudiesTrials
Benign Neoplasms
[description not available]		02.0410
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.		02.0410
Leukemia P388
An experimental lymphocytic leukemia originally induced in DBA/2 mice by painting with methylcholanthrene.		02.420
Carcinoma, Ehrlich Tumor
A transplantable, poorly differentiated malignant tumor which appeared originally as a spontaneous breast carcinoma in a mouse. It grows in both solid and ascitic forms.		0210
Neuroblastoma
A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)		02.4120