Compounds > combretastatin a-4 disodium phosphate
Page last updated: 2024-12-11

combretastatin a-4 disodium phosphate

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Cross-References

ID SourceID
PubMed CID6918309
CHEMBL ID289351
SCHEMBL ID321426
MeSH IDM0374590

Synonyms (42)

Synonym
nsc-752293
ca-4p
ca4dp
CHEMBL289351 ,
ca 4p
ca-4dp
fosbretabulin disodium salt
fosbretabulin disodium (usan)
D09346
BCP9000542
702rhr475o ,
fosbretabulin disodium [usan]
unii-702rhr475o
phenol, 2-methoxy-5-((1z)-2-(3,4,5-trimethoxyphenyl)ethenyl)-, 1-(dihydrogen phosphate), sodium salt (1:2)
combretastatin a4 disodium phosphate
168555-66-6
2-methoxy-5-[(1z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenyl disodium phosphate
phenol, 2-methoxy-5-(2-(3,4,5-trimethoxyphenyl)ethenyl)-, dihydrogen phosphate, disodium salt, (z)-
phenol, 2-methoxy-5-((1z)-2-(3,4,5-trimethoxyphenyl)ethenyl)-, dihydrogen phosphate, disodium salt
fosbretabulin disodium salt [mi]
S7204
combretastatin a4 phosphate disodium salt
SCHEMBL321426
fosbretabulin (disodium)
FD18018
AC-30267
sodium (z)-2-methoxy-5-(3,4,5-trimethoxystyryl)phenyl phosphate
mfcd00943911
AKOS027327946
fosbretabulin (combretastatin a4 phosphate (ca4p)) disodium
AS-74880
disodium 2-methoxy-5-[(1z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenyl phosphate
fosbretabulin disodium, >=98% (hplc)
disodium (z)-2-methoxy-5-(3,4,5-trimethoxystyryl)phenyl phosphate
disodium;[2-methoxy-5-[(z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenyl] phosphate
fosbretabulin (combretastatin a4 phosphate,
C3009
CCG-269118
Q27265817
A907765
2-methoxy-5-[(1z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenol 1-(dihydrogen phosphate) sodium salt ca 4p
disodium(z)-2-methoxy-5-(3,4,5-trimethoxystyryl)phenylphosphate
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Tubulin alpha-1A chainSus scrofa (pig)IC50 (µMol)40.00000.00672.160310.0000AID228626
Tubulin beta-2B chainBos taurus (cattle)IC50 (µMol)80.00000.25001.88388.7000AID214160
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)IC50 (µMol)80.00000.25001.87798.7000AID214160
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)IC50 (µMol)80.00000.25001.86568.7000AID214160
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (3)

Processvia Protein(s)Taxonomy
microtubule-based processTubulin beta-2B chainBos taurus (cattle)
nervous system developmentTubulin beta-2B chainBos taurus (cattle)
positive regulation of axon guidanceTubulin beta-2B chainBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
GTPase activityTubulin beta-2B chainBos taurus (cattle)
metal ion bindingTubulin beta-2B chainBos taurus (cattle)
protein heterodimerization activityTubulin beta-2B chainBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
microtubule cytoskeletonTubulin beta-2B chainBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (189)

Assay IDTitleYearJournalArticle
AID1613402Induction of apoptosis in human HeLa cells assessed as early apoptotic cells at 0.05 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 3.65%)
AID1064325Induction of apoptosis in human Jurkat cells assessed as active caspase 3 expression at 15 nM by FITC-conjugated flow cytometric analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID144649The compound was tested for the concentration for 50% growth inhibition of NCI 60 cell line human tumor screen.1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
AID1555137Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 1 uM measured after 10 mins by beckman scintillation counting method relative to control2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.
AID1064344Induction of apoptosis in human Jurkat cells assessed as decrease in sub-G1 phase cells at 15 nM after 24 to 48 hrs by propidium iodide staining-based flow cytometric analysis in presence of pancaspase peptide inhibitor z-VAD-fmk2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1338009Antiproliferative activity against human MDA-MB-468 cells measured after 96 hrs by Celltiter-Glo assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies.
AID1565963Antitumour activity against human A549 cells xenografted in BALB/c nude mouse assessed as tumour weight at 30 mg/kg, ip administered every other day measured at day 26 by electronic caliper method (Rvb = 1.894 g)
AID247220Growth inhibition against human pharynx FADU cell line2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID657882Growth inhibition of human DU145 cells after 48 hrs by sulforhodamine B assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID1320430Growth inhibition of HUVEC after 72 hrs by crystal violet staining-based assay2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4.
AID1315234Growth inhibition of human MDA-MB-231 cells measured after 48 hrs by MTS assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Efficient Synthesis of Glaziovianin A Isoflavone Series from Dill and Parsley Extracts and Their in Vitro/in Vivo Antimitotic Activity.
AID1437255Cytotoxicity against human K562 cells assessed as growth inhibition after 5 days by MTT assay2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Tubulin-binding dibenz[c,e]oxepines: Part 2. Structural variation and biological evaluation as tumour vasculature disrupting agents.
AID1858333Antiangiogenic activity in chicken fertilized egg chorioallantoic membrane assessed as inhibition of neovascularization at 50 uM measured after 48 hrs by microscopic analysis relative to control2022RSC medicinal chemistry, Sep-21, Volume: 13, Issue:9
New β-carboline derivatives containing imidazolium as potential VEGFR2 inhibitors: synthesis, X-ray structure, antiproliferative evaluations, and molecular modeling.
AID1320436Disruption of interphase microtubule in HUVEC assessed as change in cell shape and morphology at 250 nM preincubated for 30 mins followed by compound washout measured after 60 mins by DAPI staining-based immunofluorescence assay2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4.
AID767876Cytotoxicity against human NCI-H460 cells by SRB assay2013Journal of natural products, Sep-27, Volume: 76, Issue:9
Synthesis of a 2-aryl-3-aroyl indole salt (OXi8007) resembling combretastatin A-4 with application as a vascular disrupting agent.
AID1320447Induction of necrosis in human SW1222 cells xenografted in SCID mouse at 0.227 mmol/kg administered as single dose measured after 24 hrs by hematoxylin/eosin staining-based microscopic method2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4.
AID201133The compound was tested for the concentration to inhibit 50% of CNS SF-295 cell lines.1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
AID1183700Antitumor activity against mouse BNL 1ME A.7R.1 cells xenografted in Balb/c mouse model of syngeneic murine hepatocellular carcinoma assessed as reduction tumor growth at 5 mg/kg, ip2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID1320446Induction of HUVEC monolayer permeability assessed as increase in passage of FITC-dextran through cell monolayer at 50 nM preincubated for 30 mins followed by compound washout and addition of FITC-dextran for 30 mins by fluorescence assay2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4.
AID83950Cytotoxicity evaluated against colon cancer cell line (HT-29)2003Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9
Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4.
AID1315227Antimitotic activity in sea urchin Paracentrotus lividus L embryo assessed as induction of cleavage alteration2016Journal of natural products, 05-27, Volume: 79, Issue:5
Efficient Synthesis of Glaziovianin A Isoflavone Series from Dill and Parsley Extracts and Their in Vitro/in Vivo Antimitotic Activity.
AID1411801Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
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.
AID1690540Antiproliferative activity against human Bel-7402 cells measured after 48 hrs by SRB assay2020European journal of medicinal chemistry, Apr-01, Volume: 191Synthesis and structure-activity relationship study of water-soluble carbazole sulfonamide derivatives as new anticancer agents.
AID1064343Induction of apoptosis in human Jurkat/A4 cells assessed as decrease in sub-G1 phase cells at 150 nM after 24 to 48 hrs by propidium iodide staining-based flow cytometric analysis in presence of pancaspase peptide inhibitor z-VAD-fmk2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1555138Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 5 uM measured after 10 mins by beckman scintillation counting method relative to control2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.
AID1565964Antitumour activity against human A549 cells xenografted in BALB/c nude mouse assessed as tumour growth inhibition at 30 mg/kg, ip administered every other day measured at day 26 by electronic caliper method relative to control
AID150376The compound was tested for the concentration to inhibit 50% of leukemia P388 cell lines.1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
AID1613389Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
AID657907Inhibition of purified tubulin assembly after 20 mins2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID1197838Antiproliferative activity against human HeLa cells after 4 days by Coulter counter method2015European journal of medicinal chemistry, Mar-06, Volume: 92Boehmeriasin A as new lead compound for the inhibition of topoisomerases and SIRT2.
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).
AID421865Aqueous solubility of compound in water2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Antineoplastic agents. 578. Synthesis of stilstatins 1 and 2 and their water-soluble prodrugs.
AID403644Cytotoxicity against human SF268 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).
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).
AID1064358Cell cycle arrest in human Jurkat cells assessed as accumulation at sub-G1 phase at 15 nM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 12.2%)2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1315231Growth inhibition of human A375 cells measured after 48 hrs by MTS assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Efficient Synthesis of Glaziovianin A Isoflavone Series from Dill and Parsley Extracts and Their in Vitro/in Vivo Antimitotic Activity.
AID247255Growth inhibition against human neuroblastoma cell line (SK-N-SH)2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
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.
AID1064350Induction of apoptosis in human Jurkat cells assessed as small cell fragments with unequally segregated chromosomes enclosed by cell membrane after 48 hrs by May-Grunwald-Giemsa staining-based microscopic analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID550210Antimitotic activity against Paracentrotus lividus embryo assessed as cleavage arrest after 2.5 to 6 hrs post fertilization by sea urchin embryo assay2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Synthesis of antimitotic polyalkoxyphenyl derivatives of combretastatin using plant allylpolyalkoxybenzenes.
AID106518In vitro cytotoxicity evaluated in mouse heart endotheliaoma cell (MHEC5-T) after incubation of the cells for 1 hr2003Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9
Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4.
AID1608986Antitumour activity against mouse E0771 cells allografted in C57BL/6 mouse assessed as reduction in tumor mass at 30 mg/kg, ip administrated every other day by caliper method2019European journal of medicinal chemistry, Nov-01, Volume: 181Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.
AID1315228Antimitotic activity against sea urchin Paracentrotus lividus L embryo assessed as induction of cleavage arrest2016Journal of natural products, 05-27, Volume: 79, Issue:5
Efficient Synthesis of Glaziovianin A Isoflavone Series from Dill and Parsley Extracts and Their in Vitro/in Vivo Antimitotic Activity.
AID1382776Antiproliferative activity against human HeLa cells after 3 days by coulter counting method2018European journal of medicinal chemistry, Mar-25, Volume: 148Conformational mimetics of the α-methyl chalcone TUB091 binding tubulin: Design, synthesis and antiproliferative activity.
AID1064319Induction of apoptosis in human Jurkat/A4 cells assessed as active caspase 3 expression at 150 nM after 24 hrs by FITC-conjugated flow cytometric analysis (Rvb = 1.1%)2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1055625Cytotoxicity against human DU145 cells after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis of structurally diverse benzosuberene analogues and their biological evaluation as anti-cancer agents.
AID247232Growth inhibition against human prostate cell line (DU-145)2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID1055626Cytotoxicity against human NCI-H460 cells after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis of structurally diverse benzosuberene analogues and their biological evaluation as anti-cancer agents.
AID247231Growth inhibition against human lung-NSC NCI-H460 cell line2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID1064363Cell cycle arrest in human Jurkat/A4 cells assessed as increase in accumulation at G2/M phase at 150 nM after 24 hrs by propidium iodide staining-based flow cytometric analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1338014Antiproliferative activity against human MDA-MB-DYT2 cells measured after 96 hrs by Celltiter-Glo assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies.
AID1064337Induction of apoptosis in human Jurkat/A4 cells assessed as caspase 9 activation at 150 nM after 24 to 48 hrs by Western blotting analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID88795Evaluated for growth inhibition (anticancer activity) in 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.
AID1059956Antitumor activity against human MNNG-HOS cells xenografted in Balb/c-nu mouse assessed as reduction in tumor weight at 50 mg/kg, ip administered once every 3 days for 9 days measured after day 182013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Concise synthesis and biological evaluation of 2-Aroyl-5-amino benzo[b]thiophene derivatives as a novel class of potent antimitotic agents.
AID1651888Induction of vascular damage in mouse 4T1 cells harboring firefly luciferase reporter gene implanted BALB/C mouse assessed as reduction in light emission at 120 mg/kg, ip measured after 4 hrs by Bioluminescence imaging analysis2020Journal 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.
AID1613393Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
AID1064351Induction of apoptosis in human Jurkat cells assessed as micronuclei formation after 48 hrs by May-Grunwald-Giemsa staining-based microscopic analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID657881Growth inhibition of human KM20L2 cells after 48 hrs by sulforhodamine B assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID737075Antitumor activity against mouse BNL 1ME A.7R.1 cells xenografted in Balb/c mouse assessed as reduction in tumor growth at 5 mg/kg, ip QD for 7 days2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID1382777Antiproliferative activity against human HMEC1 cells after 4 days by coulter counting method2018European journal of medicinal chemistry, Mar-25, Volume: 148Conformational mimetics of the α-methyl chalcone TUB091 binding tubulin: Design, synthesis and antiproliferative activity.
AID481679Antimitotic activity against Paracentrotus lividus embryo assessed as cleavage arrest after 10 to 15 mins fertilization 45 to 60 mins before first mitotic cycle completeion2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Novel derivatives of 1,3,4-oxadiazoles are potent mitostatic agents featuring strong microtubule depolymerizing activity in the sea urchin embryo and cell culture assays.
AID481678Antiproliferative activity against Paracentrotus lividus embryo assessed as cleavage alteration after 10 to 15 mins fertilization 45 to 60 mins before first mitotic cycle completeion2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Novel derivatives of 1,3,4-oxadiazoles are potent mitostatic agents featuring strong microtubule depolymerizing activity in the sea urchin embryo and cell culture assays.
AID1651889Induction of vascular damage in mouse 4T1 cells harboring firefly luciferase reporter gene implanted BALB/C mouse assessed as reduction in light emission at 120 mg/kg, ip measured up to 72 hrs by Bioluminescence imaging analysis2020Journal 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.
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.
AID1064322Induction of apoptosis in human Jurkat cells assessed as active caspase 3 expression at 15 nM after 48 hrs by FITC-conjugated flow cytometric analysis (Rvb = 3.3%)2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1338011Antiproliferative activity against human MDA-MB-435 cells measured after 96 hrs by Celltiter-Glo assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies.
AID1858331Antiangiogenic activity in chicken fertilized egg chorioallantoic membrane assessed as inhibition of neovascularization at 0.5 uM measured after 48 hrs by microscopic analysis relative to control2022RSC medicinal chemistry, Sep-21, Volume: 13, Issue:9
New β-carboline derivatives containing imidazolium as potential VEGFR2 inhibitors: synthesis, X-ray structure, antiproliferative evaluations, and molecular modeling.
AID1411797Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID1613401Induction of apoptosis in human HeLa cells assessed as viable cells at 0.05 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 92.8%)
AID1538742Antitumour activity against mouse B16-BL6 cells allografted in C57BL/6 mouse assessed as reduction in tumor mass at 30 mg/kg, ip administrated every other day relative to control2019European journal of medicinal chemistry, Sep-15, Volume: 178Evaluating the effects of fluorine on biological properties and metabolic stability of some antitubulin 3-substituted 7-phenyl-pyrroloquinolinones.
AID1411802Inhibition of pig brain tubulin polymerization by spectrophotometric analysis2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID1315236Growth inhibition of human PBMC cells measured after 48 hrs by MTS assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Efficient Synthesis of Glaziovianin A Isoflavone Series from Dill and Parsley Extracts and Their in Vitro/in Vivo Antimitotic Activity.
AID550209Antimitotic activity against Paracentrotus lividus embryo assessed as cleavage alteration after 2.5 to 6 hrs post fertilization by sea urchin embryo assay2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Synthesis of antimitotic polyalkoxyphenyl derivatives of combretastatin using plant allylpolyalkoxybenzenes.
AID443467Cytotoxicity against human HeLa cells by MTT assay2009Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
Synthesis and antitumor-evaluation of cyclopropyl-containing combretastatin analogs.
AID1055627Cytotoxicity against human SKOV3 cells after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis of structurally diverse benzosuberene analogues and their biological evaluation as anti-cancer agents.
AID147801The compound was tested for the concentration to inhibit 50% of ovarian OVCAR cell lines.1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
AID1064366Cell cycle arrest in human Jurkat cells assessed as decrease in accumulation at G0/G1 phase at 15 nM after 24 hrs by propidium iodide staining-based flow cytometric analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID657879Growth inhibition of human SF268 cells after 48 hrs by sulforhodamine B assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID1613391Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
AID1595721Antitumor activity against mouse H22 cells allografted in ICR mouse assessed as reduction in tumour weight at 20 mg/kg, iv administered once per day for 21 days relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.
AID1064367Cell cycle arrest in human Jurkat cells assessed as increase in accumulation at G2/M phase at 15 nM after 24 hrs by propidium iodide staining-based flow cytometric analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1613463Antitumor activity against human HeLa cells xenografted in nude mouse assessed as tumor weight at 10 mg/kg, iv administered every other day up to 20 days (Rvb = 1.014 +/- 0.116g)
AID1458857Antitumor activity against human A549 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 30 mg/kg, ip2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID1690539Antiproliferative activity against human HepG2 cells measured after 48 hrs by SRB assay2020European journal of medicinal chemistry, Apr-01, Volume: 191Synthesis and structure-activity relationship study of water-soluble carbazole sulfonamide derivatives as new anticancer agents.
AID247233Growth inhibition against human thyroid cell line( SW 1736) 2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID330416Cytotoxicity against mouse MHEC5-T cells after 5 days by MTT assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID1338002Antiproliferative activity against human NCI60 cells measured after 48 hrs by SRB assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies.
AID1338007Antiproliferative activity against human TOV112D cells measured after 96 hrs by Celltiter-Glo assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies.
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.
AID1197840Antiproliferative activity against mouse L1210 cells after 48 hrs by Coulter counter method2015European journal of medicinal chemistry, Mar-06, Volume: 92Boehmeriasin A as new lead compound for the inhibition of topoisomerases and SIRT2.
AID550211Antimitotic activity against Paracentrotus lividus embryo assessed as embryo spinning after 0.5 to 20 hrs post dose by sea urchin embryo assay2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Synthesis of antimitotic polyalkoxyphenyl derivatives of combretastatin using plant allylpolyalkoxybenzenes.
AID512076Antitumor activity against mouse 3LL cells transplanted in to BALB/c mouse assessed as tumor growth inhibition at 100 mg/kg, ip qd for 2 days2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Identification of CKD-516: a potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
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).
AID1555132Cytotoxicity against human NCI-H460 cells assessed as growth inhibition measured after 48 hrs by SRB assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.
AID1064329Induction of apoptosis in human Jurkat cells assessed as Bcl-2 expression at 15 nM after 24 to 48 hrs Western blotting analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID330414Reduction of blood flow to tumor in MHEC5-T xenografted SCID mouse at 100 mg/kg, ip after 24 hrs2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID1550784Antiproliferative activity against human CEM cells measured after 96 hrs by Coulter counter method2019European journal of medicinal chemistry, Jun-01, Volume: 171Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop.
AID512075Antitumor activity against mouse 3LL cells transplanted in to BALB/c mouse assessed as tumor growth inhibition at 50 mg/kg, ip qd for 2 days2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Identification of CKD-516: a potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
AID1437254Inhibition of porcine tubulin assembly measured for 30 mins by UV/visible spectrophotometric method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Tubulin-binding dibenz[c,e]oxepines: Part 2. Structural variation and biological evaluation as tumour vasculature disrupting agents.
AID1612655Antitumor activity against human H22 cells xenografted in ICR mouse assessed as reduction in tumor weight at 20 mg/kg/day, iv for 21 days relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1613403Induction of apoptosis in human HeLa cells assessed as late apoptotic cells at 0.05 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 3.51%)
AID1858332Antiangiogenic activity in chicken fertilized egg chorioallantoic membrane assessed as inhibition of neovascularization at 5 uM measured after 48 hrs by microscopic analysis relative to control2022RSC medicinal chemistry, Sep-21, Volume: 13, Issue:9
New β-carboline derivatives containing imidazolium as potential VEGFR2 inhibitors: synthesis, X-ray structure, antiproliferative evaluations, and molecular modeling.
AID1320444Activation of ROCK in HUVEC assessed as phosphorylation of myosin light chain at 50 to 500 nM after 15 mins by Western blot method2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4.
AID1613394Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay
AID94880The compound was tested for the concentration to inhibit 50% of colon KM20L2 cell lines.1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
AID1555134Cytotoxicity against human SKOV3 cells assessed as growth inhibition measured after 48 hrs by SRB assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.
AID1651891Induction in necrosis in tumor of BALB/C mouse implanted with mouse 4T1 cells harboring firefly luciferase reporter gene at 120 mg/kg, ip measured after 72 to 96 hrs by hematoxylin and eosin staining based assay (Rvb = 46%)2020Journal 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.
AID1064369Cytotoxicity against human Jurkat/A4 cells assessed as cell death at 1 uM after 48 hrs by trypan blue exclusion assay relative to control2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID214184Percentage inhibition of colchicine binding to tubulin by compound was evaluated1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
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.
AID616992Antitumor activity against human MDA-MB-231 xenografted in mouse assessed as tumor growth inhibition at 150 mg/kg administered on day 1 and 52011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID1690563Antitumor activity against human HepG2 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 50 mg/kg, iv qod for 14 to 29 days relative to control2020European journal of medicinal chemistry, Apr-01, Volume: 191Synthesis and structure-activity relationship study of water-soluble carbazole sulfonamide derivatives as new anticancer agents.
AID1338006Antiproliferative activity against human Caov3 cells measured after 96 hrs by Celltiter-Glo assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies.
AID1315233Growth inhibition of human PC3 cells measured after 48 hrs by MTS assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Efficient Synthesis of Glaziovianin A Isoflavone Series from Dill and Parsley Extracts and Their in Vitro/in Vivo Antimitotic Activity.
AID146555The compound was tested for the concentration to inhibit 50% lung-NSC NCI-H460 cell lines.1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
AID1059958Antitumor activity against human MNNG-HOS cells xenografted in Balb/c-nu mouse assessed as tumor growth inhibition at 50 mg/kg, ip administered once every 3 days for 9 days measured on day 18 relative to vehicle-treated control2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Concise synthesis and biological evaluation of 2-Aroyl-5-amino benzo[b]thiophene derivatives as a novel class of potent antimitotic agents.
AID202156The compound was tested for the concentration to inhibit 50% of melanoma SK-MEL-5 cell lines.1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
AID1064349Induction of apoptosis in human Jurkat/A4 cells assessed as small cell fragments with unequally segregated chromosomes enclosed by cell membrane after 48 hrs by May-Grunwald-Giemsa staining-based microscopic analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1411796Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 assay2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID1411800Antiproliferative activity against human MCF7 cells after 72 hrs by CCK-8 assay2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID1555136Cytotoxicity against human DU145 cells assessed as growth inhibition measured after 48 hrs by SRB assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.
AID1337994Antimitotic activity in sea urchin embryo assessed as cleavage arrest exposed 8 to 15 mins after fertilization 45 to 55 mins before first mitotic cycle completion measured at 2.5 to 5.5 hrs post dose2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies.
AID128971Vascular shutdown expressed as vessel density decrease in percent of the control at the dose of 100 mg/kg2003Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9
Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4.
AID1613404Induction of apoptosis in human HeLa cells assessed as necrotic cells at 0.05 uM after 24 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.05%)
AID1315229Antimitotic activity against sea urchin Paracentrotus lividus L embryo assessed as induction of embryo spinning2016Journal of natural products, 05-27, Volume: 79, Issue:5
Efficient Synthesis of Glaziovianin A Isoflavone Series from Dill and Parsley Extracts and Their in Vitro/in Vivo Antimitotic Activity.
AID481680Cytotoxicity against Paracentrotus lividus embryo assessed as embryo spinning after 9 to 12 hrs fertilization and 0.5 to 20 hrs treatment2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Novel derivatives of 1,3,4-oxadiazoles are potent mitostatic agents featuring strong microtubule depolymerizing activity in the sea urchin embryo and cell culture assays.
AID1338008Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs by Celltiter-Glo assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies.
AID1197842Antiproliferative activity against bovine BAEC cells after 3 days by Coulter counter method2015European journal of medicinal chemistry, Mar-06, Volume: 92Boehmeriasin A as new lead compound for the inhibition of topoisomerases and SIRT2.
AID1064370Cytotoxicity against human Jurkat cells assessed as cell viability after 48 hrs by trypan blue exclusion assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID330413Reduction of blood flow to tumor in MHEC5-T xenografted SCID mouse at 10 mg/kg, ip after 24 hrs2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID657877Growth inhibition of human BxPC3 cells after 48 hrs by sulforhodamine B assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
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.
AID1315235Growth inhibition of human SKOV3 cells measured after 48 hrs by MTS assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Efficient Synthesis of Glaziovianin A Isoflavone Series from Dill and Parsley Extracts and Their in Vitro/in Vivo Antimitotic Activity.
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.
AID1613456Antitumor activity against human HeLa cells xenografted in nude mouse assessed as tumor growth inhibition at 10 mg/kg, iv administered every other day up to 20 days relative to control
AID214160The compound was tested for the concentration to inhibit 50% of tubulin polymerization.1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
AID8106The compound was tested for the concentration to inhibit 50% of renal A498 cell lines.1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
AID452612Antivascular activity in HUVEC cells assessed as change in cell shape at 1 uM after 1 hr by fluorescent-labeled high molecular weight F-dextran permeability assay2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: synthesis and biological evaluation of antivascular activity.
AID1064341Induction of apoptosis in human Jurkat cells assessed as caspase 9 activation at 15 nM after 48 hrs by Western blotting analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1064339Induction of apoptosis in human Jurkat cells assessed as caspase 2 activation at 15 nM after 24 to 48 hrs by Western blotting analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1337995Antimitotic activity in sea urchin free-swimming blastulae assessed as microtubule destabilization by measuring embryo spinning exposed 8 to 10 hrs after fertilization measured after 15 mins to 20 hrs2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies.
AID1320437Disruption of interphase microtubule in HUVEC assessed as formation of actin stress fiber at 250 nM preincubated for 30 mins followed by compound washout measured after 60 mins by DAPI staining-based immunofluorescence assay2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4.
AID330415Cytotoxicity against mouse MHEC5-T cells after 1 hr by MTT assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID657876Growth inhibition of mouse P388 cells after 48 hrs by Z1 Beckman/Coulter particle counter analysis2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID657880Growth inhibition of human NCI-H460 cells after 48 hrs by sulforhodamine B assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID1064330Induction of apoptosis in human Jurkat/A4 cells assessed as reduction of XIAP expression at 150 nM after 24 hrs Western blotting analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1055628Inhibition of calf brain tubulin polymerization after 15 mins by UV-visible spectrophotometry2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis of structurally diverse benzosuberene analogues and their biological evaluation as anti-cancer agents.
AID330417Growth inhibition of mouse P388 cells2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID1550785Antiproliferative activity against human HeLa cells measured after 3 days by Coulter counter method2019European journal of medicinal chemistry, Jun-01, Volume: 171Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop.
AID1064346Cell cycle arrest in human Jurkat/A4 cells assessed as accumulation at sub-G1 phase at 150 nM after 48 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 17.1%)2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1382775Antiproliferative activity against human CEM cells after 96 hrs by coulter counting method2018European journal of medicinal chemistry, Mar-25, Volume: 148Conformational mimetics of the α-methyl chalcone TUB091 binding tubulin: Design, synthesis and antiproliferative activity.
AID1337993Antimitotic activity in sea urchin embryo assessed as cleavage alteration exposed 8 to 15 mins after fertilization 45 to 55 mins before first mitotic cycle completion measured at 2.5 to 5.5 hrs post dose2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies.
AID1064318Induction of apoptosis in human Jurkat/A4 cells assessed as active caspase 3 expression at 150 nM after 48 hrs by FITC-conjugated flow cytometric analysis (Rvb = 1.1%)2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1550786Antiproliferative activity against mouse L1210 cells measured after 96 hrs by Coulter counter method2019European journal of medicinal chemistry, Jun-01, Volume: 171Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop.
AID1690541Antiproliferative activity against human MCF7 cells measured after 48 hrs by SRB assay2020European journal of medicinal chemistry, Apr-01, Volume: 191Synthesis and structure-activity relationship study of water-soluble carbazole sulfonamide derivatives as new anticancer agents.
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.
AID1613390Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
AID106520In vitro cytotoxicity evaluated in mouse heart endotheliaoma cell (MHEC5-T) after incubation of the cells for 5 days2003Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9
Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4.
AID1411799Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID1064327Induction of apoptosis in human Jurkat/A4 cells assessed as Bcl-2 expression at 150 nM after 24 to 48 hrs Western blotting analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
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.
AID246826Effective dose against murine P388 leukemia cell line2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID1197841Antiproliferative activity against human HMEC1 cells after 4 days by Coulter counter method2015European journal of medicinal chemistry, Mar-06, Volume: 92Boehmeriasin A as new lead compound for the inhibition of topoisomerases and SIRT2.
AID1320432Disruption of interphase microtubule in HUVEC assessed as formation of actin stress fiber at 250 nM after 30 mins by phalloidin/DAPI staining-based immunofluorescence assay2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4.
AID1197839Antiproliferative activity against human CEM cells after 96 hrs by Coulter counter method2015European journal of medicinal chemistry, Mar-06, Volume: 92Boehmeriasin A as new lead compound for the inhibition of topoisomerases and SIRT2.
AID443468Cytotoxicity against human MCF7 cells by MTT assay2009Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
Synthesis and antitumor-evaluation of cyclopropyl-containing combretastatin analogs.
AID1411798Antiproliferative activity against human HepG2 cells after 72 hrs by CCK-8 assay2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID1064333Induction of apoptosis in human Jurkat cells assessed as reduction of XIAP expression at 15 nM after 24 hrs Western blotting analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1315230Growth inhibition of human A549 cells by MTS assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Efficient Synthesis of Glaziovianin A Isoflavone Series from Dill and Parsley Extracts and Their in Vitro/in Vivo Antimitotic Activity.
AID1320431Disruption of interphase microtubule in HUVEC assessed as change in cell morphology at 250 nM after 30 mins by DAPI staining-based immunofluorescence assay2016Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20
Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4.
AID1064335Induction of apoptosis in human Jurkat/A4 cells assessed as caspase 2 activation at 150 nM after 24 to 48 hrs by Western blotting analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1064323Induction of apoptosis in human Jurkat cells assessed as active caspase 3 expression at 15 nM after 24 hrs by FITC-conjugated flow cytometric analysis (Rvb = 3.3%)2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1382774Antiproliferative activity against mouse L1210 cells after 96 hrs by coulter counting method2018European journal of medicinal chemistry, Mar-25, Volume: 148Conformational mimetics of the α-methyl chalcone TUB091 binding tubulin: Design, synthesis and antiproliferative activity.
AID1613392Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
AID247272Growth inhibition against human pancreas carcinoma cell line (BxPC-3)2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID1315232Growth inhibition of human DU145 cells measured after 48 hrs by MTS assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Efficient Synthesis of Glaziovianin A Isoflavone Series from Dill and Parsley Extracts and Their in Vitro/in Vivo Antimitotic Activity.
AID1064348Induction of apoptosis in human Jurkat/A4 cells assessed as micronuclei formation after 48 hrs by May-Grunwald-Giemsa staining-based microscopic analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1064362Cell cycle arrest in human Jurkat/A4 cells assessed as decrease in accumulation at G0/G1 phase at 150 nM after 24 hrs by propidium iodide staining-based flow cytometric analysis2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID767874Cytotoxicity against human DU145 cells by SRB assay2013Journal of natural products, Sep-27, Volume: 76, Issue:9
Synthesis of a 2-aryl-3-aroyl indole salt (OXi8007) resembling combretastatin A-4 with application as a vascular disrupting agent.
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.
AID767875Cytotoxicity against human SKOV3 cells by SRB assay2013Journal of natural products, Sep-27, Volume: 76, Issue:9
Synthesis of a 2-aryl-3-aroyl indole salt (OXi8007) resembling combretastatin A-4 with application as a vascular disrupting agent.
AID1572282Antitumor activity against mouse B16 cells allografted in C57BL/6 mouse assessed as reduction in tumor burden at 30 mg/kg, ip dosing starting on day 9 post tumor injection administered qid on day 9,11, 13 and 15 relative to control2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.
AID1315226Growth inhibition of human HCT116 cells measured after 48 hrs by MTS assay2016Journal of natural products, 05-27, Volume: 79, Issue:5
Efficient Synthesis of Glaziovianin A Isoflavone Series from Dill and Parsley Extracts and Their in Vitro/in Vivo Antimitotic Activity.
AID1205544In vivo antitumor activity against mouse BNL 1ME A.7R.1 cells allografted in Balb/c mouse assessed as reduction in tumor growth at 5 mg/kg, ip up to 8 days relative to vehicle treated control2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin.
AID1738880Antitumor activity mouse E0771 cells implanted in C57BL/6 mouse assessed as reduction tumor growth at 30 mg/kg, ip administered every other day relative to control2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, in vitro and in vivo biological evaluation of 2-amino-3-aroylbenzo[b]furan derivatives as highly potent tubulin polymerization inhibitors.
AID1338013Antiproliferative activity against human NCI-H1975 cells measured after 96 hrs by Celltiter-Glo assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis and anti-mitotic activity of 6,7-dihydro-4H-isothiazolo[4,5-b]pyridin-5-ones: In vivo and cell-based studies.
AID1550787Antiproliferative activity against human HMEC1 cells measured after 4 days by Coulter counter method2019European journal of medicinal chemistry, Jun-01, Volume: 171Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop.
AID1565962Antitumour activity against human A549 cells xenografted in BALB/c nude mouse assessed as tumour volume at 30 mg/kg, ip administered every other day measured at day 26 by electronic caliper method (Rvb = 2006.37 mm3)
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (43)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (2.33)18.2507
2000's9 (20.93)29.6817
2010's29 (67.44)24.3611
2020's4 (9.30)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.33

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 Index11.33 (24.57)
Research Supply Index3.78 (2.92)
Research Growth Index5.12 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.33)

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%
Other43 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
amsacrine
Amsacrine: An aminoacridine derivative that intercalates into DNA and is used as an antineoplastic agent.. amsacrine : A sulfonamide that is N-phenylmethanesulfonamide substituted by a methoxy group at position 3 and an acridin-9-ylamino group at position 4. It exhibits antineoplastic activity.		2.1110acridines;
aromatic ether;
sulfonamide		antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
nocodazole
[no description available]		2.0510aromatic ketone;
benzimidazoles;
carbamate ester;
thiophenes		antimitotic;
antineoplastic agent;
microtubule-destabilising agent;
tubulin modulator
myristicin
myristicin: asaricin is an isomer; structure; a methylene dioxy version of elemicin;		2.0510organic molecular entitymetabolite
vincristine
[no description available]		2.5220acetate ester;
formamides;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
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.		3.2350alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
Dillapiole
5-allyl 6,7-dimethoxy 1,3-benzodioxole: a plant based insecticide; structure in first source		2.0510benzodioxolesmetabolite
podophyllotoxin
Podophyllum: A genus of poisonous American herbs, family BERBERIDACEAE. The roots yield PODOPHYLLOTOXIN and other pharmacologically important agents. The plant was formerly used as a cholagogue and cathartic. It is different from the European mandrake, MANDRAGORA.		2.8130furonaphthodioxole;
lignan;
organic heterotetracyclic compound		antimitotic;
antineoplastic agent;
keratolytic drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
apiole
apiole: crystalline essential oil isolated directly from commercial oil of parsley		2.0510benzodioxolesmetabolite
vinblastine
[no description available]		2.7730
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		2.1110delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant 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).		3.460taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
rb 6145
RB 6145: structure given in first source; prodrug to RSU 1069; PD 144872 is the R-enantiomer of RB 6145		2.2510
methotrexate
[no description available]		2.0510dicarboxylic 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
combretastatin b-1
combretastatin B-1: structure in first source		210
erlotinib
[no description available]		2.2110aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound		antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor
sorafenib
[no description available]		2.4110(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide		angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor
erianin
Erianin: from Dendrobium chrysotoxum; structure in first source		1.9910
doxorubicin hydrochloride
[no description available]		2.2110anthracycline
chalcone
trans-chalcone : The trans-isomer of chalcone.		2.0510chalconeEC 3.2.1.1 (alpha-amylase) inhibitor
su 11248
[no description available]		2.2110monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
fosbretabulin
[no description available]		4.91330stilbenoid
1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene
[no description available]		1.9910
nsc 600032
combretastatin A-1: from Combretum caffrum; structure given in first source		3.2960
metochalcone
metochalcone: structure		2.0510
3',4',5',3,4,5-hexamethoxy-chalcone
[no description available]		2.0510
mdl 27048
MDL 27048: structure given in first source; powerful & reversible microtubule inhibitor		2.0510
combretastatin a3
combretastatin A3: RN given for (Z)-isomer; structure in first source		2.4520
ac 7700
AC 7700: a vascular disrupting agent; structure in first source		2.4620
ave-8063
AVE-8063: has both antivascular and antineoplastic activities; structure in first source		2.7330
3-hydroxy-4,3',4',5'-tetramethoxychalcone
3-hydroxy-4,3',4',5'-tetramethoxychalcone: structure in first source		2.520
3,4-methylenedioxy-3',4',5'-trimethoxy chalcone
[no description available]		2.0510
combretastatin a-2
combretastatin A-2: isolated from Combretum caffrum; RN from first source; structure given in first source		2.9840
glaziovianin a
glaziovianin A: structure in first source		2.1310
isocombretastatin a-4
[no description available]		2.1510
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
Leukemia P388
An experimental lymphocytic leukemia originally induced in DBA/2 mice by painting with methylcholanthrene.		02.9440
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.520
Benign Neoplasms
[description not available]		03.2250
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.		15.83100
Cancer of Prostate
[description not available]		02.0810
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		02.0810
Hepatocellular Carcinoma
[description not available]		02.110
Cancer of Liver
[description not available]		02.110
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.		02.110
Liver Neoplasms
Tumors or cancer of the LIVER.		02.110
Experimental Neoplasms
[description not available]		02.8830
Breast Cancer
[description not available]		02.2510
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.2510