Compounds > nsc 600032
Page last updated: 2024-12-11

nsc 600032

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Description

combretastatin A-1: from Combretum caffrum; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5458993
CHEMBL ID36255
SCHEMBL ID8736882
MeSH IDM0175754

Synonyms (32)

Synonym
b8173373k297
nsc-600032
NSC600032 ,
combretastatin a-1
(z)-3-(3,4,5-trimethoxystyryl)-6-methoxybenzene-1,2-diol
3-methoxy-6-[(z)-2-(3,4,5-trimethoxyphenyl)vinyl]benzene-1,2-diol
(z)-2'',3''-dihydroxy-3,4,4'',5-tetramethoxystilbene
combretastatins a-1
3-methoxy-6-[(z)-2-(3,4,5-trimethoxy-phenyl)-vinyl]-benzene-1,2-diol
3-methoxy-6-[2-(3,4,5-trimethoxy-phenyl)-vinyl]-benzene-1,2-diol
bdbm50090044
oxi4500
CHEMBL36255 ,
combretastatin a1
3-methoxy-6-[(z)-2-(3,4,5-trimethoxyphenyl)ethenyl]benzene-1,2-diol
3-methoxy-6-[(e)-2-(3,4,5-trimethoxyphenyl)vinyl]benzene-1,2-diol
109971-63-3
A802119
2222ats339 ,
nsc 600032
unii-2222ats339
1,2-benzenediol, 3-methoxy-6-(2-(3,4,5-trimethoxyphenyl)ethenyl)-, (z)-
AKOS022180052
combretastatin a-1 [mi]
combretastatin a1 [who-dd]
SCHEMBL8736882
(z)-3-methoxy-6-(3,4,5-trimethoxystyryl)benzene-1,2-diol
1,2-benzenediol,3-methoxy-6-[(1z)-2-(3,4,5-trimethoxyphenyl)ethenyl]-
MS-24999
HY-121993
DTXSID701028842
CS-0083815

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"Although in vitro studies suggest that variable rates of tumor-specific prodrug dephosphorylation may explain these differences in pharmacokinetics profiles, the improved antitumor activity and altered pharmacokinetic profile of CA1 may be due to the formation of a more reactive metabolite."( Comparative preclinical pharmacokinetic and metabolic studies of the combretastatin prodrugs combretastatin A4 phosphate and A1 phosphate.
Anthoney, DA; Bibby, MC; Cooper, PA; Kirwan, IG; Lippert, JW; Loadman, PM; Pettit, GR; Shnyder, SD; Swaine, DJ, 2004)		0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Tubulin alpha-1A chainSus scrofa (pig)IC50 (µMol)2.30000.00672.160310.0000AID228626; AID635032
Tubulin beta chainSus scrofa (pig)IC50 (µMol)3.50000.00672.137410.0000AID635032
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (86)

Assay IDTitleYearJournalArticle
AID635028Cytotoxicity against human HT-29 cells by alamar blue assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID421860Antitumor activity against human NCI-H460 cells by sulforhodamine B assay2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Antineoplastic agents. 578. Synthesis of stilstatins 1 and 2 and their water-soluble prodrugs.
AID480731Cell cycle arrest in Saccharomyces cerevisiae BY4741 assessed as accumulation of cells at metaphase with short spindles by FACS analysis2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
AID611594Inhibition of tubulin polymerization in bovine brain after 20 mins by spectrophotometry2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Regioselective synthesis of water-soluble monophosphate derivatives of combretastatin A-1.
AID611593Cytotoxicity against human DU145 cells by SRB assay2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Regioselective synthesis of water-soluble monophosphate derivatives of combretastatin A-1.
AID337715Displacement of [3H]colchicine from tubulin after 10 mins relative to control
AID1651876Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 1 uM incubated for 10 mins by scintillation counting relative to control2020Journal of natural products, 04-24, Volume: 83, Issue:4
Bioreductively Activatable Prodrug Conjugates of Combretastatin A-1 and Combretastatin A-4 as Anticancer Agents Targeted toward Tumor-Associated Hypoxia.
AID147019Antimicrobial activity against Neisseria gonorrhoeae1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID330411Cytotoxicity against human KM20L2 cells after 48 hrs by SRB assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID379680Inhibition of topoisomerase 1 in Saccharomyces cerevisiae RS321N in galactose medium by microtiter plate assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID228627Inhibition of colchicine binding2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID611591Cytotoxicity against human SKOV3 cells by SRB assay2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Regioselective synthesis of water-soluble monophosphate derivatives of combretastatin A-1.
AID635030Cytotoxicity against human fibroblast cells by alamar blue assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID338991Antimitotic activity in mouse L1210 cells assessed as increase in mitotic index at 2 to 7 times IC50 after 6 hrs relative to control
AID337712In vivo cytotoxicity against mouse P388 cells assessed as increase in life extension at 2.75 to 11 mg/kg
AID338987Displacement of [3H]colchicine from tubulin at inhibitor and colchicine ratio 1:1 after 10 mins relative to control
AID403641Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID379682Inhibition of Saccharomyces cerevisiae RS188 expressing wild type erg6 by agar diffusion assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID330407Cytotoxicity against human BXPC3 cells after 48 hrs by SRB assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID379678Inhibition of pRAD52 recombination repair gene/topoisomerase 1 deficient Saccharomyces cerevisiae RS321N carrying pRAD52 in galactose medium by microtiter plate assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID228626Inhibition of tubulin polymerization2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID1651883Cytotoxicity against human A549 cells incubated for 4 hrs in anoxic condition followed by oxic exposure for 48 hrs by sulforhodamine B assay2020Journal of natural products, 04-24, Volume: 83, Issue:4
Bioreductively Activatable Prodrug Conjugates of Combretastatin A-1 and Combretastatin A-4 as Anticancer Agents Targeted toward Tumor-Associated Hypoxia.
AID355284Inhibition of adenosine diphosphate-induced platelet aggregation in human platelet-rich plasma1997Journal of natural products, Nov, Volume: 60, Issue:11
Isolation, synthesis, and antiplatelet aggregation activity of resveratrol 3-O-beta-D-glucopyranoside and related compounds.
AID421857Antitumor activity against human BxPC3 cells by sulforhodamine B assay2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Antineoplastic agents. 578. Synthesis of stilstatins 1 and 2 and their water-soluble prodrugs.
AID376520Cytotoxicity against mouse P388 cells2000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID644559Antivascular activity against HUVEC cells assessed as cell growth inhibition after 48 hrs by xCELLigence assay2012Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5
Increased endothelial cell selectivity of triazole-bridged dihalogenated A-ring analogues of combretastatin A-1.
AID330410Cytotoxicity against human NCIH460 cells after 48 hrs by SRB assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID403642Cytotoxicity against human BxPC3 cells after 48 hrs by sulforhodamine B assay2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID12681Half-life in rat serum2003Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5
An adjustable release rate linking strategy for cytotoxin-peptide conjugates.
AID337713In vivo cytotoxicity against mouse P388 cells
AID644558Antivascular activity against HUVEC cells assessed as cell growth inhibition after 24 hrs by xCELLigence assay2012Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5
Increased endothelial cell selectivity of triazole-bridged dihalogenated A-ring analogues of combretastatin A-1.
AID376521Cytotoxicity against human FaDu cells2000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID376523Inhibition of bovine tubulin polymerization2000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID421862Antitumor activity against human DU145 cells by sulforhodamine B assay2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Antineoplastic agents. 578. Synthesis of stilstatins 1 and 2 and their water-soluble prodrugs.
AID403647Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID1651882Cytotoxicity against human A549 cells incubated for 52 hrs in oxic condition by sulforhodamine B assay2020Journal of natural products, 04-24, Volume: 83, Issue:4
Bioreductively Activatable Prodrug Conjugates of Combretastatin A-1 and Combretastatin A-4 as Anticancer Agents Targeted toward Tumor-Associated Hypoxia.
AID90279In vitro antitumor activity against human tumor cancer cell lines1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Antineoplastic agents. 291. Isolation and synthesis of combretastatins A-4, A-5, and A-6(1a)
AID379677Inhibition of Saccharomyces cerevisiae RS321NYCp50 in galactose medium by microtiter plate assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID224778Evaluated for growth inhibition (anticancer activity) of human pancreas-a BXPC-3 cell line.2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID338990Cytotoxicity against mouse L1210 cells after 24 hrs
AID397287Cytotoxicity against human NCI60 cells2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Isocombretastatins a versus combretastatins a: the forgotten isoCA-4 isomer as a highly promising cytotoxic and antitubulin agent.
AID337714Inhibition of microtubule assembly by turbidimetry
AID338988Displacement of [3H]colchicine from tubulin at inhibitor and colchicine ratio 10:1 after 10 mins relative to control
AID379679Inhibition of pRAD52 recombination repair gene/topoisomerase 1 deficient Saccharomyces cerevisiae RS321N carrying pRAD52 in glucose medium by microtiter plate assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID1119741Growth inhibition of human NCI-H460 cells by sulforhodamine B assay2012MedChemComm, Jun, Volume: 3, Issue:6
An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.
AID330412Cytotoxicity against human DU145 cells after 48 hrs by SRB assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID1119739Displacement of [3H]-Colchicine from tubulin (unknown origin) at 5 uM relative to control2012MedChemComm, Jun, Volume: 3, Issue:6
An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.
AID376526Antibacterial activity against Staphylococcus aureus by disk susceptibility test2000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID403646Cytotoxicity against human KM20L2 cells after 48 hrs by sulforhodamine B assay2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID379684Inhibition of Saccharomyces cerevisiae RS322 expressing Rad52.erg6 by agar diffusion assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID26178Half-life in phosphate buffer; na is not available2003Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5
An adjustable release rate linking strategy for cytotoxin-peptide conjugates.
AID635027Cytotoxicity against human NCI-H460 cells by alamar blue assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID1651877Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 5 uM incubated for 10 mins by scintillation counting relative to control2020Journal of natural products, 04-24, Volume: 83, Issue:4
Bioreductively Activatable Prodrug Conjugates of Combretastatin A-1 and Combretastatin A-4 as Anticancer Agents Targeted toward Tumor-Associated Hypoxia.
AID91554Cytotoxic activity against human neuroblastoma IMR32 cells which over-express somatostatin receptors; na is not active2003Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5
An adjustable release rate linking strategy for cytotoxin-peptide conjugates.
AID93448Evaluated for growth inhibition (anticancer activity) of Human prostate cancer DU-145 cell line2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID379683Inhibition of Saccharomyces cerevisiae RS321 expressing Rad52.erg6.top1 by agar diffusion assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID142305Evaluated for growth inhibition (anticancer activity) of Murine P388 lymphocytic leukemia cell line2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID89699Evaluated for growth inhibition (anticancer activity) of Human CNS cancer SF-295 cell line2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID363250Growth inhibition of human SK-OV-3 after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Design, synthesis and biological evaluation of dihydronaphthalene and benzosuberene analogs of the combretastatins as inhibitors of tubulin polymerization in cancer chemotherapy.
AID611592Cytotoxicity against human NCI-H460 cells by SRB assay2011Journal of natural products, Jul-22, Volume: 74, Issue:7
Regioselective synthesis of water-soluble monophosphate derivatives of combretastatin A-1.
AID486868Inhibition of bovine brain tubulin assembly after 20 mins2010Journal of natural products, Jun-25, Volume: 73, Issue:6
Regio- and stereospecific synthesis of mono-beta-d-glucuronic acid derivatives of combretastatin A-1.
AID376525Displacement of [3H]colchicine from bovine tubulin at inhibitor to colchicine ratio of 1:12000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID330406Inhibition of calf tubulin polymerization2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID1119740Displacement of [3H]-Colchicine from tubulin (unknown origin) at 1 uM relative to control2012MedChemComm, Jun, Volume: 3, Issue:6
An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.
AID355281Inhibition of collagen-induced platelet aggregation in human platelet-rich plasma1997Journal of natural products, Nov, Volume: 60, Issue:11
Isolation, synthesis, and antiplatelet aggregation activity of resveratrol 3-O-beta-D-glucopyranoside and related compounds.
AID1119743Growth inhibition of human SKOV3 cells by sulforhodamine B assay2012MedChemComm, Jun, Volume: 3, Issue:6
An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.
AID379681Inhibition of topoisomerase 1 in Saccharomyces cerevisiae RS321N in glucose medium by microtiter plate assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID486869Cytotoxicity against human DU145 cells by SRB assay2010Journal of natural products, Jun-25, Volume: 73, Issue:6
Regio- and stereospecific synthesis of mono-beta-d-glucuronic acid derivatives of combretastatin A-1.
AID486871Cytotoxicity against human NCI-H460 cells by SRB assay2010Journal of natural products, Jun-25, Volume: 73, Issue:6
Regio- and stereospecific synthesis of mono-beta-d-glucuronic acid derivatives of combretastatin A-1.
AID1119742Growth inhibition of human DU145 cells by sulforhodamine B assay2012MedChemComm, Jun, Volume: 3, Issue:6
An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.
AID480723Induction of log phase growth arrest in Saccharomyces cerevisiae BY47412010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
AID635031Inhibition of angiogenesis in endothelial cells assessed as inhibition of tube formation after 18 hrs by inverted microscopic analysis2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID421856In vivo antitumor activity against mouse P388 cells2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Antineoplastic agents. 578. Synthesis of stilstatins 1 and 2 and their water-soluble prodrugs.
AID338986Inhibition of microtubule assembly after 15 mins
AID363249Growth inhibition of human DU145 after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Design, synthesis and biological evaluation of dihydronaphthalene and benzosuberene analogs of the combretastatins as inhibitors of tubulin polymerization in cancer chemotherapy.
AID363248Growth inhibition of human NCI-H460 after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Design, synthesis and biological evaluation of dihydronaphthalene and benzosuberene analogs of the combretastatins as inhibitors of tubulin polymerization in cancer chemotherapy.
AID480724Cell cycle arrest in Saccharomyces cerevisiae BY4741 assessed as accumulation of cells at metaphase with post synthetic DNA content by FACS analysis2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
AID635026Cytotoxicity against human MCF7 cells by alamar blue assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID207493Antimicrobial activity against Staphylococcus aureus1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID403645Cytotoxicity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID376524Displacement of [3H]colchicine from bovine tubulin at inhibitor to colchicine ratio of 0.2:12000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID635029Cytotoxicity against human CEM cells by alamar blue assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID635032Inhibition of porcine brain tubulin polymerization after 60 mins2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID376527Antibacterial activity against Neisseria gonorrhoeae by disk susceptibility test2000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID90436Evaluated for growth inhibition (anticancer activity) of Human colon KM20L2 cancer cell line2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID196070Inhibitory activity against GHRH-stimulated GH release from monolayer cultures of rat pituitary cells2003Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5
An adjustable release rate linking strategy for cytotoxin-peptide conjugates.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (35)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (11.43)18.2507
2000's15 (42.86)29.6817
2010's14 (40.00)24.3611
2020's2 (5.71)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 (%)
Trials1 (2.38%)5.53%
Reviews1 (2.38%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other40 (95.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
guaiacol
Guaiacol: An agent thought to have disinfectant properties and used as an expectorant. (From Martindale, The Extra Pharmacopoeia, 30th ed, p747). methylcatechol : Any member of the class of catechols carrying one or more methyl substituents.. guaiacol : A monomethoxybenzene that consists of phenol with a methoxy substituent at the ortho position.		210guaiacolsdisinfectant;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
expectorant;
plant metabolite
pyrazole
1H-pyrazole : The 1H-tautomer of pyrazole.		2.0810pyrazole
pyruvic acid
Pyruvic Acid: An intermediate compound in the metabolism of carbohydrates, proteins, and fats. In thiamine deficiency, its oxidation is retarded and it accumulates in the tissues, especially in nervous structures. (From Stedman, 26th ed). pyruvic acid : A 2-oxo monocarboxylic acid that is the 2-keto derivative of propionic acid. It is a metabolite obtained during glycolysis.		2.15102-oxo monocarboxylic acidcofactor;
fundamental metabolite
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.		2.5120alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
cytarabine
[no description available]		3.6411beta-D-arabinoside;
monosaccharide derivative;
pyrimidine nucleoside		antimetabolite;
antineoplastic agent;
antiviral agent;
immunosuppressive agent
thiazoles
[no description available]		2.02101,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
gadolinium
Gadolinium: An element of the rare earth family of metals. It has the atomic symbol Gd, atomic number 64, and atomic weight 157.25. Its oxide is used in the control rods of some nuclear reactors.		2.1510f-block element atom;
lanthanoid atom
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		2.0110delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
daunorubicin
Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola.		1.9710aminoglycoside antibiotic;
anthracycline;
p-quinones;
tetracenequinones		antineoplastic agent;
bacterial metabolite
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		2.0210taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
thiazolyl blue
thiazolyl blue: RN & II refers to bromide. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide : The bromide salt of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium.		2.0210organic bromide saltcolorimetric reagent;
dye
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		2.48201,2,3-triazole
glucuronic acid
Glucuronic Acid: A sugar acid formed by the oxidation of the C-6 carbon of GLUCOSE. In addition to being a key intermediate metabolite of the uronic acid pathway, glucuronic acid also plays a role in the detoxification of certain drugs and toxins by conjugating with them to form GLUCURONIDES.. D-glucuronic acid : The D-enantiomer of glucuronic acid.. D-glucopyranuronic acid : A D-glucuronic acid in cyclic pyranose form.		2.0510D-glucuronic acidalgal metabolite
combretastatin
combretastatin: cytotoxic principle from South African tree COMBRETUM caffrum; structure given in first source; acts at COLCHICINE site of TUBULIN		2.4120
rb 6145
RB 6145: structure given in first source; prodrug to RSU 1069; PD 144872 is the R-enantiomer of RB 6145		2.2510
combretastatin b-1
combretastatin B-1: structure in first source		2.9340
glycosides
[no description available]		210
stilbenes
Stilbenes: Organic compounds that contain 1,2-diphenylethylene as a functional group.. trans-stilbene : The trans-isomer of stilbene.		7.02231stilbene
pyrophosphate
Diphosphates: Inorganic salts of phosphoric acid that contain two phosphate groups.		3.8921diphosphate ion
polydatin
trans-piceid : A stilbenoid that is trans-resveratrol substituted at position 3 by a beta-D-glucosyl residue.		1.9910beta-D-glucoside;
monosaccharide derivative;
polyphenol;
stilbenoid		anti-arrhythmia drug;
antioxidant;
geroprotector;
hepatoprotective agent;
metabolite;
nephroprotective agent;
potassium channel modulator
desoxyrhaponticin
[no description available]		1.9910glycoside;
stilbenoid
fosbretabulin
[no description available]		4.23170stilbenoid
fosbretabulin
fosbretabulin: a microtubule destabilizing agent isolated from Combretum caffrum; structure in first source		4.3960
3,5-dihydroxy-4'-methoxystilbene
4'-methoxyresveratrol: has anti-inflammatory effects in cell culture model		1.9910
combretastatin a3
combretastatin A3: RN given for (Z)-isomer; structure in first source		2.4420
combretastatin a-4 disodium phosphate
[no description available]		3.2960
oxi 4503
Oxi 4503: diphosphate prodrug of cambretastatin A1		3.8921
ave-8063
AVE-8063: has both antivascular and antineoplastic activities; structure in first source		2.0510
combretastatin a-2
combretastatin A-2: isolated from Combretum caffrum; RN from first source; structure given in first source		2.7130
isocombretastatin a-4
[no description available]		2.0510
ascorbic acid
Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms.		2.0310ascorbic acid;
vitamin C		coenzyme;
cofactor;
flour treatment agent;
food antioxidant;
food colour retention agent;
geroprotector;
plant metabolite;
skin lightening agent
transforming growth factor beta
Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.		2.1310
tirapazamine
Tirapazamine: A triazine derivative that introduces breaks into DNA strands in hypoxic cells, sensitizing tumor cells to the cytotoxic activity of other drugs and radiation.. tirapazamine : A member of the class of benzotriazines that is 1,2,4-benzotriazine carrying an amino substituent at position 3 and two oxido substituents at positions 1 and 4.		2.2510aromatic amine;
benzotriazines;
N-oxide		antibacterial agent;
antineoplastic agent;
apoptosis inducer
ConditionIndicatedRelationship StrengthStudiesTrials
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)		02.0110
Leukemia P388
An experimental lymphocytic leukemia originally induced in DBA/2 mice by painting with methylcholanthrene.		03.1250
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.0410
Benign Neoplasms
[description not available]		02.7630
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.		02.7630
Cancer of Ovary
[description not available]		02.0710
Ovarian Neoplasms
Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.		02.0710
Breast Cancer
[description not available]		02.2510
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.2510
Bleeding
[description not available]		03.6411
Dysmyelopoietic Syndromes
[description not available]		03.6411
Acute Respiratory Distress Syndrome
[description not available]		03.6411
Acute Myelogenous Leukemia
[description not available]		03.6411
Hemorrhage
Bleeding or escape of blood from a vessel.		03.6411
Myelodysplastic Syndromes
Clonal hematopoietic stem cell disorders characterized by dysplasia in one or more hematopoietic cell lineages. They predominantly affect patients over 60, are considered preleukemic conditions, and have high probability of transformation into ACUTE MYELOID LEUKEMIA.		03.6411
Respiratory Distress Syndrome
A syndrome characterized by progressive life-threatening RESPIRATORY INSUFFICIENCY in the absence of known LUNG DISEASES, usually following a systemic insult such as surgery or major TRAUMA.		03.6411
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.		03.6411
Metastase
[description not available]		03.4520
Angiogenesis, Pathologic
[description not available]		03.4120
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		15.4520
Hepatocellular Carcinoma
[description not available]		02.1310
Cancer of Liver
[description not available]		02.1310
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		02.1310
Liver Neoplasms
Tumors or cancer of the LIVER.		02.1310