Assay ID | Title | Year | Journal | Article |
AID1472802 | Inhibition of human RRM2 expressed in Escherichia coli BL21-codon plus(DE3) using [14C]-ADP as substrate after 3 mins by liquid scintillation counting method | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
| Structure-Guided Synthesis and Mechanistic Studies Reveal Sweetspots on Naphthyl Salicyl Hydrazone Scaffold as Non-Nucleosidic Competitive, Reversible Inhibitors of Human Ribonucleotide Reductase. |
AID127872 | Average survival days at the dose 20x2 mg/ kg in mice bearing the L1210 Leukemia | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID135608 | Effect on administering twice daily at a dose of 10x2 mg/kg expressed as long term survivors (>60 days); 4/10 | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID350247 | Selectivity ratio of IC50 for human P-gp-negative KB-3-1 cells to human P-glycoprotein-expressing KBV1 cells | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
AID1319026 | Induction of lysosomal membrane permeabilization in human KB3-1 cells at 10 uM after 30 mins by acridine orange staining based fluorescence microscopic analysis | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance. |
AID1319020 | Antiproliferative activity against human KBV1 cells over expressing P-gp after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance. |
AID1626669 | Cytotoxicity against human A2780 cells pre-incubated with CuCl2 for 60 mins followed by compound addition for for 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention. |
AID1626662 | Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention. |
AID1319018 | Antiproliferative activity against human KB3-1 cells after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance. |
AID1692153 | Antiproliferative activity against human MGC-803 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Thiosemicarbazone-based lead optimization to discover high-efficiency and low-toxicity anti-gastric cancer agents. |
AID136233 | Effect of compound on mice bearing the L1210 Leukemia expressed as T/C percent treated/control)-dose 40 mg/ kg | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1735983 | Antagonistic antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability at 0.05 to 1000 nM incubated for 48 hrs in presence of copper by cell-titer-Glo luminescent based Chou-Talay method | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID312544 | Antiproliferative activity against human SK-MN-C cells by MTT assay | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of novel iron chelators for the treatment of iron overload disease: the methyl pyrazinylketone isonicotinoyl hydrazone series. |
AID135614 | Effect on administering twice daily at a dose of 20x2 mg/kg expressed as long term survivors (>60 days); 1/10 | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1692161 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Thiosemicarbazone-based lead optimization to discover high-efficiency and low-toxicity anti-gastric cancer agents. |
AID1692155 | Selectivity index, ratio of IC50 for cytotoxicity against human GES1 to IC50 for antiproliferative activity against human MGC-803 cells | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Thiosemicarbazone-based lead optimization to discover high-efficiency and low-toxicity anti-gastric cancer agents. |
AID127723 | Average change in body weight from onset to termination of therapy in mice bearing the L1210 Leukemia(dose 30x2 mg/ kg ) | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID350249 | Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
AID1735948 | Induction of mitochondrial membrane potential loss in human MV4-11 cells measured at 8 to 24 hrs by JC1 staining based FACScalibur flow cytometry analysis | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1735891 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1692159 | Antiproliferative activity against human EC9706 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Thiosemicarbazone-based lead optimization to discover high-efficiency and low-toxicity anti-gastric cancer agents. |
AID1626661 | Resistance factor, ratio of IC50 for triapine-resistant human SW480 cells to IC50 for human SW480 cells incubated for 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention. |
AID350248 | Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
AID1728309 | Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis and biological evaluation of novel thiosemicarbazone-indole derivatives targeting prostate cancer cells. |
AID1711815 | Cytotoxicity against human MES-SA cells transfected with mCherry fluorescent protein assessed as inhibition of cell proliferation incubated for 72 hrs by fluorescent assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and biological evaluation of thiosemicarbazones, hydrazinobenzothiazoles and arylhydrazones as anticancer agents with a potential to overcome multidrug resistance. |
AID1610251 | Antiproliferative activity against human PC3 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Novel thiosemicarbazone derivatives containing indole fragment as potent and selective anticancer agent. |
AID1735886 | Antiproliferative activity against human KG-1a cells assessed as reduction in cell viability at 0.1 to 100 uM incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID127873 | Average survival days at the dose 30x2 mg/ kg in mice bearing the L1210 Leukemia | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1692157 | Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Thiosemicarbazone-based lead optimization to discover high-efficiency and low-toxicity anti-gastric cancer agents. |
AID345783 | Inhibition of human recombinant ribonucleotide reductase expressed in BL21 (DE3) bacteria assessed as conversion of [3H]CDP to [3H]dCDP | 2008 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
| Synthesis and ribonucleotide reductase inhibitory activity of thiosemicarbazones. |
AID1319021 | Antiproliferative activity against human KBV1 cells over expressing P-gp after 24 hrs in presence of P-gp inhibitor elacridar by MTT assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance. |
AID1626660 | Cytotoxicity against triapine-resistant human SW480 cells incubated for 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention. |
AID1692160 | Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Thiosemicarbazone-based lead optimization to discover high-efficiency and low-toxicity anti-gastric cancer agents. |
AID136228 | Effect of compound on mice bearing the L1210 Leukemia expressed as T/C percent treated/control)-dose 10x2 mg/ kg | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID8330 | Compound was evaluated for area under the curve in dog blood. | 1998 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
| Synthesis and biological evaluation of a water soluble phosphate prodrug of 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP). |
AID439762 | Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
| Thiosemicarbazones from the old to new: iron chelators that are more than just ribonucleotide reductase inhibitors. |
AID127722 | Average change in body weight from onset to termination of therapy in mice bearing the L1210 Leukemia(dose 20x2 mg/ kg ) | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1735882 | Metal chelating activity assessed as copper chelation by UV-Visible spectrophotometry | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1735895 | Intrinsic clearance mouse in liver microsomes at 10 uM preincubated for 5 mins followed by NADPH addition and measured up to 45 mins by LC/MS analysis | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1626658 | Cytotoxicity against human A2780 cells incubated for 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention. |
AID1626671 | Induction of intracellular ROS generation in human HL60 cells at 1 and 5 uM in presence of CuCl2 incubated for 30 mins by DCF-DA staining based fluorescence assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention. |
AID1416716 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2017 | MedChemComm, Dec-01, Volume: 8, Issue:12
| Thiosemicarbazone-based selective proliferation inactivators inhibit gastric cancer cell growth, invasion, and migration. |
AID1735892 | Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID722568 | Toxicity in human RBC lysates assessed as methemoglobin formation at 25 uM after 3 hrs (Rvb = 1.2 +/- 8%) | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Alkyl substituted 2'-benzoylpyridine thiosemicarbazone chelators with potent and selective anti-neoplastic activity: novel ligands that limit methemoglobin formation. |
AID1728310 | Antiproliferative activity against human ECa-109 cell line cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis and biological evaluation of novel thiosemicarbazone-indole derivatives targeting prostate cancer cells. |
AID127720 | Average change in body weight from onset to termination of therapy in mice bearing the L1210 Leukemia(dose 15x2 mg/ kg ) | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1319019 | Antiproliferative activity against human KB3-1 cells after 24 hrs in presence of P-gp inhibitor elacridar by MTT assay | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance. |
AID1735888 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability at 0.1 to 100 uM incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID292406 | Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Design, synthesis, and characterization of novel iron chelators: structure-activity relationships of the 2-benzoylpyridine thiosemicarbazone series and their 3-nitrobenzoyl analogues as potent antitumor agents. |
AID1735945 | Upregulation of TXNIP protein expression in human MV4-11 cells at 50 nM incubated for 24 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID127719 | Average change in body weight from onset to termination of therapy in mice bearing the L1210 Leukemia(dose 10x2 mg/ kg ) | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1626663 | Cytotoxicity against human KBC1 cells incubated for 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention. |
AID1151101 | Photocytotoxicity against human HCT116 cells expressing wild type p53 assessed as combination index incubated for 24 hrs followed by light irradiation measured after 24 hrs by MTS assay in presence of ALA | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
| Iron chelators in photodynamic therapy revisited: synergistic effect by novel highly active thiosemicarbazones. |
AID1550506 | Growth inhibition of mouse L1210 cells by MTS assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Multi-target compounds acting in cancer progression: Focus on thiosemicarbazone, thiazole and thiazolidinone analogues. |
AID1735944 | Upregulation of TXNIP mRNA expression in human MV4-11 cells at 50 nM incubated for 24 hrs by qRT-PCR analysis | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1728313 | Antiproliferative activity against human MCF7 cell line cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis and biological evaluation of novel thiosemicarbazone-indole derivatives targeting prostate cancer cells. |
AID103146 | In vivo antitumor activity evaluated against M-109 murine lung carcinoma cells in BALB/c mice administered intraperitoneally at a dose of 4.5 mg/kg | 1998 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
| Synthesis and biological evaluation of a water soluble phosphate prodrug of 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP). |
AID127871 | Average survival days at the dose 15x2 mg/ kg in mice bearing the L1210 Leukemia | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1416714 | Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay | 2017 | MedChemComm, Dec-01, Volume: 8, Issue:12
| Thiosemicarbazone-based selective proliferation inactivators inhibit gastric cancer cell growth, invasion, and migration. |
AID1735986 | Upregulation of TXNIP protein expression in human MV4-11 cells at 500 nM incubated for 24 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1711816 | Cytotoxicity against human MES-SA/DX5 cells transfected with mCherry fluorescent protein assessed as inhibition of cell proliferation incubated for 72 hrs by fluorescent assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and biological evaluation of thiosemicarbazones, hydrazinobenzothiazoles and arylhydrazones as anticancer agents with a potential to overcome multidrug resistance. |
AID127874 | Average survival days at the dose 40 mg/ kg in mice bearing the L1210 Leukemia | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1416715 | Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay | 2017 | MedChemComm, Dec-01, Volume: 8, Issue:12
| Thiosemicarbazone-based selective proliferation inactivators inhibit gastric cancer cell growth, invasion, and migration. |
AID722565 | Toxicity in intact human RBC assessed as methemoglobin formation at 25 uM after 3 hrs relative to untreated control | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Alkyl substituted 2'-benzoylpyridine thiosemicarbazone chelators with potent and selective anti-neoplastic activity: novel ligands that limit methemoglobin formation. |
AID127870 | Average survival days at the dose 10x2 mg/ kg in mice bearing the L1210 Leukemia | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1692158 | Antiproliferative activity against human BGC-823 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Thiosemicarbazone-based lead optimization to discover high-efficiency and low-toxicity anti-gastric cancer agents. |
AID1735985 | Metal chelating activity assessed as ferric chelation by UV-Visible spectrophotometry | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1610255 | Antiproliferative activity against human GES-1 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Novel thiosemicarbazone derivatives containing indole fragment as potent and selective anticancer agent. |
AID439766 | Antitumor activity against mouse M109 cells implanted in CD2F1 hybrid mouse assessed as reduction of tumor weight at 6 mg/kg, iv administered 4 days after implantation BID for 5 days measured on day 12 after implantation relative to control | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
| Thiosemicarbazones from the old to new: iron chelators that are more than just ribonucleotide reductase inhibitors. |
AID1319028 | Induction of ROS accumulation in human KBV1 cells over expressing P-gp at 10 uM after 30 mins by DCF-DA staining based flow cytometry | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance. |
AID1735893 | Selectivity index, ratio of IC50 for HUVEC to IC50 for human MV4-11 cells | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID293115 | Antiproliferative activity against human SK-N-MC cells by MTT assay | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Investigating biological activity spectrum for novel quinoline analogues. |
AID135615 | Effect on administering twice daily at a dose of 30x2 mg/kg expressed as long term survivors (>60 days); 0/5 | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1323834 | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Identification of small molecules that bind to the mitochondrial protein mitoNEET. |
AID1735987 | Induction of JNK phosphorylation in human MV4-11 cells at 500 nM incubated for 24 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1711821 | Cytotoxicity against human MES-SA/DX5 cells incubated for 72 hrs in presence of efflux pump inhibitor, Tariquidar by MTT assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and biological evaluation of thiosemicarbazones, hydrazinobenzothiazoles and arylhydrazones as anticancer agents with a potential to overcome multidrug resistance. |
AID1735936 | Synergistic antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability at 0.05 to 1000 nM incubated for 48 hrs in presence of copper by cell-titer-Glo luminescent based Chou-Talay method | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1735887 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability at 0.1 to 100 uM incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1735921 | Induction of ROS generation in human MV4-11 cells assessed as increase in mitochondrial ROS level incubated for 4 to 8 hrs by MitoSox red dye based flow cytometry analysis | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1692154 | Cytotoxicity against human GES1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Thiosemicarbazone-based lead optimization to discover high-efficiency and low-toxicity anti-gastric cancer agents. |
AID1728312 | Antiproliferative activity against human MGC-803 cell line cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis and biological evaluation of novel thiosemicarbazone-indole derivatives targeting prostate cancer cells. |
AID303515 | Antiproliferative activity against human MRC5 cells by MTT assay | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
| Design, synthesis, and characterization of new iron chelators with anti-proliferative activity: structure-activity relationships of novel thiohydrazone analogues. |
AID1626666 | Induction of morphological changes in human SW480 cells assessed as induction of massive cell flattening at 2.5 uM incubated for 48 hrs by phase contrast microscopy | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention. |
AID1416717 | Cytotoxicity against human GES-1 cells after 72 hrs by MTT assay | 2017 | MedChemComm, Dec-01, Volume: 8, Issue:12
| Thiosemicarbazone-based selective proliferation inactivators inhibit gastric cancer cell growth, invasion, and migration. |
AID1728311 | Antiproliferative activity against human DU-145 cell line cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis and biological evaluation of novel thiosemicarbazone-indole derivatives targeting prostate cancer cells. |
AID1151106 | Photocytotoxicity against human HCT116 cells expressing wild type p53 incubated for 24 hrs followed by light irradiation measured after 24 hrs by MTS assay in presence of ALA and FeCl3 | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
| Iron chelators in photodynamic therapy revisited: synergistic effect by novel highly active thiosemicarbazones. |
AID1626665 | Cytotoxicity against human WI38 cells incubated for 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention. |
AID1626657 | n-octanol/water distribution coefficient, log D in pH 7.4 HEPES buffer at 0.10M KCl by shake-flask method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention. |
AID136229 | Effect of compound on mice bearing the L1210 Leukemia expressed as T/C percent treated/control)-dose 15x2 mg/ kg | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1323835 | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
| Identification of small molecules that bind to the mitochondrial protein mitoNEET. |
AID1692156 | Antiproliferative activity against human HGC-27 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | Thiosemicarbazone-based lead optimization to discover high-efficiency and low-toxicity anti-gastric cancer agents. |
AID1319027 | Induction of lysosomal membrane permeabilization in human KBV1 cells over expressing P-gp at 10 uM after 30 mins by acridine orange staining based fluorescence microscopic analysis | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance. |
AID1626659 | Cytotoxicity against human SW480 cells incubated for 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention. |
AID127724 | Average change in body weight from onset to termination of therapy in mice bearing the L1210 Leukemia(dose 40 mg/ kg ) | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID439764 | Toxicity in iv dosed CD2F1 hybrid mouse assessed as maximum tolerated dose administered BID at an interval of 6 hrs for 5 days a week over 2 weeks | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
| Thiosemicarbazones from the old to new: iron chelators that are more than just ribonucleotide reductase inhibitors. |
AID303514 | Antiproliferative activity against human SK-N-MC cells by MTT assay | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
| Design, synthesis, and characterization of new iron chelators with anti-proliferative activity: structure-activity relationships of novel thiohydrazone analogues. |
AID722572 | Induction of 59Fe efflux in human SK-N-MC cells prelabeled with 59Fe2-Tf at 25 uM after 3 hrs by gamma-scintillation counting analysis (Rvb = 5 +/- 1%) | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Alkyl substituted 2'-benzoylpyridine thiosemicarbazone chelators with potent and selective anti-neoplastic activity: novel ligands that limit methemoglobin formation. |
AID1735984 | Metal chelating activity assessed as ferrous chelation by UV-Visible spectrophotometry | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID136231 | Effect of compound on mice bearing the L1210 Leukemia expressed as T/C percent treated/control)-dose 20x2 mg/ kg | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1610254 | Antiproliferative activity against human WPMY-1 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Novel thiosemicarbazone derivatives containing indole fragment as potent and selective anticancer agent. |
AID9542 | Compound was evaluated for plasma clearance. | 1998 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
| Synthesis and biological evaluation of a water soluble phosphate prodrug of 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP). |
AID1735883 | Antiproliferative activity against human KMS-11 cells assessed as reduction in cell viability at 0.1 to 100 uM incubated for 48 hrs by cell-titer-Glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1151096 | Dark cytotoxicity against human HCT116 cells expressing wild type p53 after 96 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
| Iron chelators in photodynamic therapy revisited: synergistic effect by novel highly active thiosemicarbazones. |
AID1151109 | Induction of ROS generation in human HCT116 cells expressing wild type p53 at 4 uM after 24 hrs by spectrophotometry | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
| Iron chelators in photodynamic therapy revisited: synergistic effect by novel highly active thiosemicarbazones. |
AID136232 | Effect of compound on mice bearing the L1210 Leukemia expressed as T/C percent treated/control)-dose 30x2 mg/ kg | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID722571 | Reduction of cellular 59Fe uptake from 59Fe-Transferrin in human SK-N-MC cells assessed as 59Fe level prelabeled with 59Fe2-Tf at 25 uM after 3 hrs relative to control | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Alkyl substituted 2'-benzoylpyridine thiosemicarbazone chelators with potent and selective anti-neoplastic activity: novel ligands that limit methemoglobin formation. |
AID1735894 | Half life in mouse liver microsomes at 10 uM preincubated for 5 mins followed by NADPH addition and measured up to 45 mins by LC/MS analysis | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID1610261 | Selectivity index, ratio of IC50 for human GES-1 cells to IC50 for human PC3 cells incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Novel thiosemicarbazone derivatives containing indole fragment as potent and selective anticancer agent. |
AID1319023 | Substrate activity at P-gp (unknown origin) in P-gp enriched membranes assessed as increase in ATPase activity at 50 uM in presence of Mg2-ATP after 40 mins by luciferase reporter gen assay relative to control | 2016 | Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
| Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance. |
AID1626664 | Resistance factor, ratio of IC50 for human KBC1 cells to IC50 for human KB-3-1 cells incubated for 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention. |
AID1610260 | Selectivity index, ratio of IC50 for human WPMY-1 cells to IC50 for human PC3 cells incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Novel thiosemicarbazone derivatives containing indole fragment as potent and selective anticancer agent. |
AID1735988 | Induction of p38 phosphorylation in human MV4-11 cells at 500 nM incubated for 24 hrs by Western blot analysis | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Novel Triapine Derivative Induces Copper-Dependent Cell Death in Hematopoietic Cancers. |
AID135612 | Effect on administering twice daily at a dose of 15x2 mg/kg expressed as long term survivors (>60 days); 0/5 | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
| Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone. |
AID1728314 | Cytotoxicity against human WPMY-1 cell line cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Design, synthesis and biological evaluation of novel thiosemicarbazone-indole derivatives targeting prostate cancer cells. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |