| Assay ID | Title | Year | Journal | Article |
|---|
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1432709 | Metabolic stability in rat liver microsomes assessed as esterase-mediated amide bond hydrolysis at 2 uM measured up to 150 mins by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1399592 | Stability in rat plasma at 1 uM after 20 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1391243 | Antiproliferative activity against human BxPC3 cells after 72 hrs by sulforhodamine B assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Design, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure. |
| AID1713025 | Cytotoxicity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1399611 | Inhibition of CYP2C19 in human liver microsomes preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1399604 | Stability in rat liver microsomes at 50 uM after 150 mins in presence of NADPH by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1713045 | Induction of apoptosis in human U-937 cells assessed as late apoptotic cells cells at 0.015 uM measured after 24 hrs by annexinV/FITC-propidium iodide staining based flow cytometry (Rvb = 2.18 to 2.22 %) | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1156703 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
| AID1594326 | Antiproliferative activity in human NCI-H1975 cells assessed as inhibition of cell proliferation at 6.25 nM incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1453843 | Drug level treated with Sodium (S)-2-(4-(4-((((3Z,6Z)-6-benzylidene-3-((5-(tertbutyl)-1H-imidazol-4-yl)methylene)-5-oxo-3,4,5,6-tetrahydropyrazin-2-yl)oxy)methoxy)-4-oxobutyl)-1H-1,2,3-triazol-1-yl)succinate assessed as porcine liver carboxylic-ester hydr | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Click strategy using disodium salts of amino acids improves the water solubility of plinabulin and KPU-300. |
| AID1594340 | Toxicity in human A549 cells xenografted Balb/c nude mouse assessed as body weight change weight at 6 mg/kg, iv dosed on day 0, 3, 6, 9, 12, 15 and 18 regime (Rvb = 6.96%) | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID628581 | Cytotoxicity against human HT-29 cells | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
| Highlights of marine invertebrate-derived biosynthetic products: their biomedical potential and possible production by microbial associants. |
| AID1156705 | Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
| AID1432711 | Half life in Wistar rat at 5 mg/kg, iv | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1168956 | Inhibition of mitotic spindle formation in human HeLa cells at 20 to 70 nM by DAPI staining | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Development of a new benzophenone-diketopiperazine-type potent antimicrotubule agent possessing a 2-pyridine structure. |
| AID1399614 | Protein binding in human plasma at 2 uM after 4 hrs by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1594317 | Antiproliferative activity in human A549 cells assessed as inhibition of cell proliferation at 1.5625 nM incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1653720 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by SRB assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Development of novel phenoxy-diketopiperazine-type plinabulin derivatives as potent antimicrotubule agents based on the co-crystal structure. |
| AID1594331 | Antitumor activity activity against human A549 cells xenografted in Balb/c nude mouse assessed as tumor volume at 12 mg/kg, iv dosed as Q3D x 3 weeks regime relative to untreated control | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1399591 | Stability in rat plasma at 1 uM after 10 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1594329 | Antiproliferative activity in human NCI-H1975 cells assessed as inhibition of cell proliferation at 50 nM incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1713043 | Induction of apoptosis in human U-937 cells assessed as viable cells at 0.015 uM measured after 24 hrs by annexinV/FITC-propidium iodide staining based flow cytometry (Rvb = 95 to 95.1 %) | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1432708 | Metabolic stability in rat plasma assessed as esterase-mediated amide bond hydrolysis at 1 uM measured up to 100 mins by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1399602 | Stability in rat liver microsomes at 50 uM after 90 mins in presence of NADPH by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID659043 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 30 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 16.2 %) | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID480334 | Cytotoxicity against human HT-29 cells | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| Anti-microtubule 'plinabulin' chemical probe KPU-244-B3 labeled both alpha- and beta-tubulin. |
| AID1399590 | Stability in rat plasma at 1 uM after 5 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1594328 | Antiproliferative activity in human NCI-H1975 cells assessed as inhibition of cell proliferation at 25 nM incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID658916 | Binding affinity to bovine tubulin after 1 hr by spectrofluorometric analysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1653722 | Inhibition of porcine brain tubulin polymerization at 5 uM by fluorescence analysis relative to control | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Development of novel phenoxy-diketopiperazine-type plinabulin derivatives as potent antimicrotubule agents based on the co-crystal structure. |
| AID659055 | Antitumor activity against human DU145 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 3.75 mg/kg, ip administered on day 1, 3, 5, 8 and 11 measured on day 40 relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1713067 | Induction of apoptosis in human U-937 cells assessed as apoptotic ratio at 0.015 uM measured after 24 hrs by annexinV/FITC-propidium iodide staining based flow cytometry (Rvb = 3.7 +/- 0.3 %) | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1668215 | Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10
| Structure-based design and synthesis of novel furan-diketopiperazine-type derivatives as potent microtubule inhibitors for treating cancer. |
| AID1594327 | Antiproliferative activity in human NCI-H1975 cells assessed as inhibition of cell proliferation at 12.5 nM incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID659045 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at S phase at 100 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 39.9 %) | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID658923 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G0/G1 phase at 30 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 43.9 %) | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID670888 | Cytotoxicity against human HT-29 cells after 48 hrs by resazurin assay | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents. |
| AID1399609 | Inhibition of CYP1A2 in human liver microsomes preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1432716 | Observed apparent volume of distribution in Wistar rat at 5 mg/kg, iv | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1594336 | Antitumor activity activity against human A549 cells xenografted in Balb/c nude mouse assessed as tumor weight at 6 mg/kg, iv dosed as Q3D x 3 weeks regime (Rvb = 0.596 +/- 0.042 g) | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1713059 | Induction of apoptosis in human U-937 cells assessed as viable cells at 0.015 uM measured after 48 hrs by annexinV/FITC-propidium iodide staining based flow cytometry (Rvb = 93.7 to 94.2 %) | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1594324 | Antiproliferative activity in human NCI-H1975 cells assessed as inhibition of cell proliferation at 1.5625 nM incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1432715 | Observed AUC (0 to infinity) in Wistar rat at 5 mg/kg, iv | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1399608 | Clearance in rat liver microsomes at 50 uM in presence of NADPH by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1594321 | Antiproliferative activity in human A549 cells assessed as inhibition of cell proliferation at 25 nM incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1713062 | Induction of apoptosis in human U-937 cells assessed as necrotic cells cells at 0.015 uM measured after 48 hrs by annexinV/FITC-propidium iodide staining based flow cytometry (Rvb = 0.794 to 0.955 %) | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID658918 | Binding affinity to porcine tubulin after 1 hr by spectrofluorometric analysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID480335 | Binding affinity to pig tubulin after 1 hr by fluorescence quenching analysis | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| Anti-microtubule 'plinabulin' chemical probe KPU-244-B3 labeled both alpha- and beta-tubulin. |
| AID1168947 | Inhibition of porcine tubulin polymerization by spectrophotometry | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Development of a new benzophenone-diketopiperazine-type potent antimicrotubule agent possessing a 2-pyridine structure. |
| AID1156701 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
| AID1156708 | Cytotoxicity against human U937 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
| AID1594320 | Antiproliferative activity in human A549 cells assessed as inhibition of cell proliferation at 12.5 nM incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1399599 | Stability in rat liver microsomes at 50 uM after 20 mins in presence of NADPH by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1399607 | Half life in rat liver microsomes at 50 uM in presence of NADPH by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID659050 | Cytotoxicity against HUVEC after 48 hrs using resazurin by microplate fluorometer analysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1713044 | Induction of apoptosis in human U-937 cells assessed as early apoptotic cells cells at 0.015 uM measured after 24 hrs by annexinV/FITC-propidium iodide staining based flow cytometry (Rvb = 1.28 to 1.68 %) | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1399597 | Stability in rat liver microsomes at 50 uM after 5 mins in presence of NADPH by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID551512 | Cytotoxicity against human HT-29 cells after 72 hrs by XTT/PMS method | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
| Tubulin photoaffinity labeling study with a plinabulin chemical probe possessing a biotin tag at the oxazole. |
| AID1399612 | Inhibition of CYP2D6 in human liver microsomes preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1594318 | Antiproliferative activity in human A549 cells assessed as inhibition of cell proliferation at 3.125 nM incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1399605 | Stability in rat liver microsomes at 50 uM after 210 mins in presence of NADPH by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1432712 | Tmax in Wistar rat at 5 mg/kg, iv | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1653723 | Inhibition of tubulin polymerization in human NCI-H460 cells assessed as formation of spindle formation at 5 nM after 24 hrs by DAPI staining based confocal microscopic analysis | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Development of novel phenoxy-diketopiperazine-type plinabulin derivatives as potent antimicrotubule agents based on the co-crystal structure. |
| AID1713060 | Induction of apoptosis in human U-937 cells assessed as early apoptotic cells cells at 0.015 uM measured after 48 hrs by annexinV/FITC-propidium iodide staining based flow cytometry (Rvb = 1.78 to 1.88 %) | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID658919 | Inhibition of bovine brain tubulin polymerization by thermostatic spectrophotometer | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1668216 | Inhibition of tubulin in human NCI-H460 cells assessed as inhibition of microtubule polymerization at 10 nM after 24 hrs by immunofluorescence assay | 2020 | Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10
| Structure-based design and synthesis of novel furan-diketopiperazine-type derivatives as potent microtubule inhibitors for treating cancer. |
| AID1168949 | Cytotoxicity against human A549 cells after 48 hrs by WST8 assay | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Development of a new benzophenone-diketopiperazine-type potent antimicrotubule agent possessing a 2-pyridine structure. |
| AID1432710 | Elimination rate constant in Wistar rat at 5 mg/kg, iv | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1432719 | Cytotoxicity against human NCI-H460 cells assessed as decrease in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1391242 | Solubility of the compound in water after 24 hrs by HPLC analysis | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Design, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure. |
| AID1156707 | Cytotoxicity against human MOLT4 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
| AID1453845 | Drug level treated with Sodium (S)-2-(4-(4-((((3Z,6Z)-6-benzylidene-3-((5-(tertbutyl)-1H-imidazol-4-yl)methylene)-5-oxo-3,4,5,6-tetrahydropyrazin-2-yl)oxy)methoxy)-4-oxobutyl)-1H-1,2,3-triazol-1-yl)pentanedioate assessed as porcine liver carboxylic-ester | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Click strategy using disodium salts of amino acids improves the water solubility of plinabulin and KPU-300. |
| AID1668213 | Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10
| Structure-based design and synthesis of novel furan-diketopiperazine-type derivatives as potent microtubule inhibitors for treating cancer. |
| AID1399594 | Stability in rat plasma at 1 uM after 60 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID659056 | Antitumor activity against human DU145 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 7.5 mg/kg, ip administered on day 1, 3, 5, 8 and 11 measured on day 40 relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1594312 | Inhibition of tubulin (unknown origin) polymerization at 5 uM | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1432717 | Observed clearance in Wistar rat at 5 mg/kg, iv | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1399593 | Stability in rat plasma at 1 uM after 40 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1399613 | Inhibition of CYP3A4 in human liver microsomes preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1432714 | AUClast in Wistar rat at 5 mg/kg, iv | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1399596 | Stability in rat plasma at 1 uM after 120 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1713024 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1156699 | Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
| AID1713023 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID658921 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at S phase at 10 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 39.9 %) | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1594339 | Toxicity in human A549 cells xenografted Balb/c nude mouse assessed as body weight change weight at 12 mg/kg, iv dosed on day 0, 3, 6, 9, 12, 15 and 18 regime (Rvb = 6.96%) | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1156706 | Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
| AID659042 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at S phase at 30 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 39.9 %) | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1399606 | Stability in rat liver microsomes at 50 uM after 270 mins in presence of NADPH by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1713022 | Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1391244 | Inhibition of tubulin polymerization (unknown origin) at 5 uM after 1 min in presence of GTP by fluorescence-based assay relative to control | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Design, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure. |
| AID1168957 | Induction of multipolar spindle formation in human HeLa cells at 20 to 30 nM by DAPI staining | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Development of a new benzophenone-diketopiperazine-type potent antimicrotubule agent possessing a 2-pyridine structure. |
| AID659052 | Antitumor activity against human DU145 cells xenografted in nu/nu mouse assessed as tumor growth inhibition administered on day 1, 3, 5, 8 and 11 measured on day 40 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1399615 | Protein binding in Beagle dog plasma at 2 uM after 4 hrs by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID659057 | Ratio of combretastatin A-4 IC50 to compound IC50 for HUVEC | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID658917 | Cytotoxicity against human HT-29 cells after 48 hrs using resazurin by microplate fluorometer analysis | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1713026 | Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1594322 | Antiproliferative activity in human A549 cells assessed as inhibition of cell proliferation at 50 nM incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1399601 | Stability in rat liver microsomes at 50 uM after 60 mins in presence of NADPH by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1432720 | Cytotoxicity against human NCI-H446 cells assessed as decrease in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1713061 | Induction of apoptosis in human U-937 cells assessed as late apoptotic cells cells at 0.015 uM measured after 48 hrs by annexinV/FITC-propidium iodide staining based flow cytometry (Rvb = 3.27 to 3.41 %) | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1156700 | Cytotoxicity against human BGC823 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
| AID1594314 | Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1594325 | Antiproliferative activity in human NCI-H1975 cells assessed as inhibition of cell proliferation at 3.125 nM incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1594335 | Antitumor activity activity against human A549 cells xenografted in Balb/c nude mouse assessed as tumor weight at 12 mg/kg, iv dosed as Q3D x 3 weeks regime (Rvb = 0.596 +/- 0.042 g) | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID659053 | Toxicity in in nu/nu mouse assessed as weight loss at 1.25 to 7.5 mg/kg, ip after 40 days | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1432713 | Cmax in Wistar rat at 5 mg/kg, iv | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1713020 | Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1668214 | Cytotoxicity against human BxPC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10
| Structure-based design and synthesis of novel furan-diketopiperazine-type derivatives as potent microtubule inhibitors for treating cancer. |
| AID1432718 | MRTlast in Wistar rat at 5 mg/kg, iv | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1432721 | Cytotoxicity against human Jurkat cells assessed as decrease in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 27, Issue:6
| Development of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1399616 | Protein binding in Sprague-Dawley rat plasma at 2 uM after 4 hrs by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1653719 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Development of novel phenoxy-diketopiperazine-type plinabulin derivatives as potent antimicrotubule agents based on the co-crystal structure. |
| AID1391245 | Inhibition of beta-tubulin polymerization in human BxPC3 cells at 5 nM after 24 hrs by DAPI staining-based fluorescence microscopic analysis | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| Design, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure. |
| AID659051 | Induction of microtubule depolymerization in HUVEC after 30 mins by DAPI staining method | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1156702 | Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
| AID658920 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G0/G1 phase at 10 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 43.9 %) | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID658922 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 10 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 16.2 %) | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1399595 | Stability in rat plasma at 1 uM after 90 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1713021 | Cytotoxicity against human HL-60 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1594332 | Antitumor activity activity against human A549 cells xenografted in Balb/c nude mouse assessed as tumor volume at 6 mg/kg, iv dosed as Q3D x 3 weeks regime relative to untreated control | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1453836 | Solubility of the compound in water | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
| Click strategy using disodium salts of amino acids improves the water solubility of plinabulin and KPU-300. |
| AID1653718 | Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by SRB assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Development of novel phenoxy-diketopiperazine-type plinabulin derivatives as potent antimicrotubule agents based on the co-crystal structure. |
| AID1168946 | Binding affinity to porcine tubulin incubated for 1 hr by spectrofluorometry | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Development of a new benzophenone-diketopiperazine-type potent antimicrotubule agent possessing a 2-pyridine structure. |
| AID1594313 | Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1594319 | Antiproliferative activity in human A549 cells assessed as inhibition of cell proliferation at 6.25 nM incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
| Polymorphs, co-crystal structure and pharmacodynamics study of MBRI-001, a deuterium-substituted plinabulin derivative as a tubulin polymerization inhibitor. |
| AID1399598 | Stability in rat liver microsomes at 50 uM after 10 mins in presence of NADPH by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID1399610 | Inhibition of CYP2C9 in human liver microsomes preincubated for 10 mins followed by NADPH addition measured after 10 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID659044 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G0/G1 phase at 100 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 43.9 %) | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1653717 | Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by SRB assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Development of novel phenoxy-diketopiperazine-type plinabulin derivatives as potent antimicrotubule agents based on the co-crystal structure. |
| AID1713068 | Induction of apoptosis in human U-937 cells assessed as apoptotic ratio at 0.015 uM measured after 48 hrs by annexinV/FITC-propidium iodide staining based flow cytometry (Rvb = 5.2 +/- 0.2 %) | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1168948 | Cytotoxicity against human HeLa cells after 48 hrs by WST8 assay | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Development of a new benzophenone-diketopiperazine-type potent antimicrotubule agent possessing a 2-pyridine structure. |
| AID659054 | Antitumor activity against human DU145 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 1.25 mg/kg, ip administered on day 1, 3, 5, 8 and 11 measured on day 40 relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1653721 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by SRB assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Development of novel phenoxy-diketopiperazine-type plinabulin derivatives as potent antimicrotubule agents based on the co-crystal structure. |
| AID1399600 | Stability in rat liver microsomes at 50 uM after 40 mins in presence of NADPH by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID659046 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 100 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 16.2 %) | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure. |
| AID1713046 | Induction of apoptosis in human U-937 cells assessed as necrotic cells cells at 0.015 uM measured after 24 hrs by annexinV/FITC-propidium iodide staining based flow cytometry (Rvb = 1.12 to 1.48 %) | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1713019 | Cytotoxicity against human U-937 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives. |
| AID1156704 | Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents. |
| AID1399603 | Stability in rat liver microsomes at 50 uM after 120 mins in presence of NADPH by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent. |
| AID551510 | Binding affinity to porcine tubulin after 1 hr by spectrofluorometric analysis | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
| Tubulin photoaffinity labeling study with a plinabulin chemical probe possessing a biotin tag at the oxazole. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |