Assay ID | Title | Year | Journal | Article |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID443471 | Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID1673980 | Antiproliferative activity against human HCT-8 cells incubated for 36 hrs | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
AID214181 | Percentage inhibition of [3H]colchicine binding site on tubulin at 5 uM | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic |
AID120695 | Compound was evaluated for the antitumor activity against P388 lymphocytic leukemia in mice | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
| Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
AID100330 | In vivo antitumor activity against L1210 intraperitoneally implanted L1210 leukemia cells; reproducible minimal activity | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
| Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
AID1694407 | Antiproliferative activity against human LoVo cells incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
AID1694415 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase after 24 to 74 hrs at 5 times of IC50 by propidium iodide staining-based flow cytometric analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
AID211307 | In vitro activity against mammalian topoisomerase II measured as ATP-dependent unknotting of P4 DNA compared to enzyme and DNA control; Inactive | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
| Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors. |
AID443478 | Cytotoxicity against c-myc/c-raf double transgenic mouse A2C12 cells by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID1527072 | Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
AID1809653 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Synthesis of thiocolchicine amine derivatives and evaluation of their antiproliferative activity. |
AID1694413 | Cell cycle arrest in human ALL-5 cells assessed as accumulation at sub-G1 phase after 48 hrs at 5 times of IC50 by propidium iodide staining-based flow cytometric analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
AID117073 | Lethal dose after the intraperitoneal injection in a group of 10 mice | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
| Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
AID23461 | Partition coefficient (logP) | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
| Quantitative structure-activity relationships of colchicines against P388 leukemia in mice. |
AID1414052 | Antifungal activity against Penicillium funiculosum BAM22 ATCC 11797 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10
| 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
AID514410 | Cytotoxicity against human SKBR3 cells after 2 days | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
AID109716 | Antitumor activity against P388 lymphocytic leukemia in mice | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
| Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
AID445542 | Cell cycle arrest in human IGROV1 cells assessed as accumulation at mitotic phase at IC80 concentration after 24 hrs using propidium iodide staining by fluorescence microscopy relative to control | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
| Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds. |
AID1627660 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Chemical synthesis, pharmacological evaluation and in silico analysis of new 2,3,3a,4,5,6-hexahydrocyclopenta[c]pyrazole derivatives as potential anti-mitotic agents. |
AID3332 | In vivo antitumor activity against 3MBG5 subrenal capsule mammary carcinoma MX-1 xenograft; NT= Not tested | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
| Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
AID1694409 | Resistance index, ratio of IC50 for antiproliferative activity against human Lovo/DX cells to IC50 for antiproliferative activity against human LoVo cells | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
AID514412 | Cytotoxicity against human KBVIN cells expressing p-glycoprotein after 2 days | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
AID408414 | Disruption of microtubule organization in human A549 cells at 10 uM after 24 hrs by immunofluorescence analysis | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
| Inhibitors of tubulin polymerization: synthesis and biological evaluation of hybrids of vindoline, anhydrovinblastine and vinorelbine with thiocolchicine, podophyllotoxin and baccatin III. |
AID1809656 | Cytotoxicity against mouse BALB/3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Synthesis of thiocolchicine amine derivatives and evaluation of their antiproliferative activity. |
AID1527073 | Antiproliferative activity against human LoVo cells assessed as reduction in cell viability | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
AID23448 | Partition coefficient (logP) | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5
| Toxicity quantitative structure--activity relationships of colchicines. |
AID136913 | In vivo antitumor activity against P388 mouse leukemia expressed as T/C (median survival time of treated animals / median survival time of untreated controls x 100) at a dose of 0.18 mg/kg | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
| A novel synthesis of colchicide and analogues from thiocolchicine and congeners: reevaluation of colchicide as a potential antitumor agent. |
AID214167 | Inhibition of radiolabeled Colchicine binding to tubulin at 37 degrees C (1.0 mM MgCl2) | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
| Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions. |
AID408416 | Inhibition of pig brain tubulin polymerization assessed as ratio of unpolymerized to polymerized tubulin at 5 uM | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
| Inhibitors of tubulin polymerization: synthesis and biological evaluation of hybrids of vindoline, anhydrovinblastine and vinorelbine with thiocolchicine, podophyllotoxin and baccatin III. |
AID514409 | Cytotoxicity against human DU145 cells after 2 days | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
AID214002 | Concentration required to inhibit the extent of glutamate-dependent tubulin polymerization by 50% at 37 degrees C(1.0 mM MgCl2) | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
| Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions. |
AID443488 | Cytotoxicity against c-myc/c-raf double transgenic mouse Craf/Cmyc cells by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID8461 | Cytotoxicity against human solid tumor lung carcinoma A549 cell line | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic |
AID1694408 | Antiproliferative activity against doxorubicin-resistant human LoVo/DX cells incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
AID1527075 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
AID1414054 | Antifungal activity against Penicillium cyclopium Westling after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10
| 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
AID214892 | Binding affinity towards tubulin protein measured by their ability to displace [3H]colchicine from rat brain at the dose 2.5 M | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
| Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
AID1527074 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
AID1627658 | Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Chemical synthesis, pharmacological evaluation and in silico analysis of new 2,3,3a,4,5,6-hexahydrocyclopenta[c]pyrazole derivatives as potential anti-mitotic agents. |
AID80380 | Cytotoxicity against human solid tumor Colon carcinoma HCT-8 cell line | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic |
AID443486 | Cytotoxicity against c-myc/c-raf double transgenic mouse yA3 cells by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID54295 | Inhibition of tubulin polymerization was determined at 1.2 mg/mL concentration | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Synthesis, anticancer activity, and inhibition of tubulin polymerization by conformationally restricted analogues of lavendustin A. |
AID1414051 | Antifungal activity against Paecilomyces variotii BAM19 ATCC 18502 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10
| 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
AID443469 | Cytotoxicity against human A549 cells after 24 hrs by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID98510 | In vitro cytotoxicity against L1210 (murine leukemia) cells. | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
| Antitubulin effects of derivatives of 3-demethylthiocolchicine, methylthio ethers of natural colchicinoids, and thioketones derived from thiocolchicine. Comparison with colchicinoids. |
AID132966 | In vivo antitumor activity against P388 mouse leukemia and minimum affective dose (MED) which produced a T/C greater than the threshold value of 125 was reported. | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
| A novel synthesis of colchicide and analogues from thiocolchicine and congeners: reevaluation of colchicide as a potential antitumor agent. |
AID445540 | Antiproliferative activity against human IGROV1 cells assessed as growth inhibition after 72 hrs by Coulter counting analysis | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
| Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds. |
AID514406 | Displacement [3H]colchicine from tubulin at 50 uM | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
AID95523 | Cytotoxicity against human solid tumor nasopharyngeal carcinoma KB cell line | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic |
AID492476 | Inhibition of tubulin polymerization | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3
| Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach. |
AID214166 | Inhibition of radiolabeled Colchicine binding to tubulin at 30 degrees C (0.25 mM MgCl2) | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
| Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions. |
AID214887 | Inhibition of tubulin polymerization interacting at the colchicine binding site. | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
| Antitumor agents. 199. Three-dimensional quantitative structure-activity relationship study of the colchicine binding site ligands using comparative molecular field analysis. |
AID443472 | Inhibition of bovine brain tubulin polymerization assessed as polymerized to unpolymerized ratio preincubated 15 mins before GTP addition measured after 30 mins by densitometry (Rvb= 1.82 +/- 0.06) | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID514408 | Cytotoxicity against human A549 cells after 2 days | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
AID1673977 | Antiproliferative activity against mouse P388 cells incubated for 36 hrs | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
AID167041 | Cytotoxicity against human melanoma RPMI-7951 cell line | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic |
AID443479 | Cytotoxicity against c-myc/c-raf double transgenic mouse yB8 cells by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID1694404 | Antiproliferative activity against human ALL5 cells incubated for 120 hrs followed by MTT addition further incubated for 48 hrs | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
AID1627661 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Chemical synthesis, pharmacological evaluation and in silico analysis of new 2,3,3a,4,5,6-hexahydrocyclopenta[c]pyrazole derivatives as potential anti-mitotic agents. |
AID445544 | Induction of apoptosis in human IGROV1 cells at IC80 concentration by TUNEL assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
| Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds. |
AID54322 | Evaluated for the stimulation of GTP hydrolysis | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic |
AID514405 | Displacement [3H]colchicine from tubulin at 5 uM | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
AID1414053 | Antifungal activity against Trichoderma viride Pers after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10
| 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
AID443484 | Cytotoxicity against c-myc/c-raf double transgenic mouse A2B1 cells by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID214893 | Binding affinity towards tubulin protein measured by their ability to displace [3H]colchicine from rat brain at the dose 25 uM | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
| Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
AID3278 | In vivo antitumor activity against 3B131 intraperitoneally implanted B16 melanoma cells; NT= Not tested | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
| Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
AID514407 | Cytotoxicity against human HCT8 cells after 2 days | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
AID443487 | Cytotoxicity against c-myc/c-raf double transgenic mouse B3 cells by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID1809655 | Antiproliferative activity against human Lovo/DX cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Synthesis of thiocolchicine amine derivatives and evaluation of their antiproliferative activity. |
AID1694405 | Antiproliferative activity against human A549 cells incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
AID1673976 | Antiproliferative activity against human KB cells incubated for 36 hrs | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
AID1673979 | Antiproliferative activity against human RPMI-7951 cells incubated for 36 hrs | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
AID1809654 | Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Synthesis of thiocolchicine amine derivatives and evaluation of their antiproliferative activity. |
AID1673974 | Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
AID214332 | Inhibitory effect on the polymerization of purified bovine brain tubulin. | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
| Antitubulin effects of derivatives of 3-demethylthiocolchicine, methylthio ethers of natural colchicinoids, and thioketones derived from thiocolchicine. Comparison with colchicinoids. |
AID1673994 | Inhibition of tubulin polymerization (unknown origin) incubated for 20 mins | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
AID134556 | Compound was tested for toxicity in non tumored mice | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5
| Toxicity quantitative structure--activity relationships of colchicines. |
AID514404 | Inhibition of tubulin assembly | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
AID103890 | Anti tumor activity on human breast cancer cell line MDR-positive MCF-7 ADRr after 72 hours of treatment | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25
| N-deacetyl-N-aminoacylthiocolchicine derivatives: synthesis and biological evaluation on MDR-positive and MDR-negative human cancer cell lines. |
AID443482 | Cytotoxicity against c-myc/c-raf double transgenic mouse betaD10 cells by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID1673975 | Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM incubated for 10 mins relative to control | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
AID42665 | Ability to inhibit Tubulin polymerization in Bovine brain | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
| Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization. |
AID134555 | Compound was tested for toxicity in P388 tumored mice | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5
| Toxicity quantitative structure--activity relationships of colchicines. |
AID443485 | Cytotoxicity against c-myc/c-raf double transgenic mouse yA7 cells by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID443480 | Cytotoxicity against c-myc/c-raf double transgenic mouse yD12 cells by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID445543 | Cell cycle arrest in human IGROV1 cells assessed as accumulation at sub-G1 phase at IC80 concentration after 24 hrs using propidium iodide staining by FACS analysis | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
| Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds. |
AID214548 | In vitro inhibition of mammalian tubulin polymerization by 50% | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
| Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors. |
AID337172 | Cytotoxicity against human H9 cells | | | |
AID91689 | In vitro inhibition of tubulin polymerization. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
| Antitumor agents. 141. Synthesis and biological evaluation of novel thiocolchicine analogs: N-acyl-, N-aroyl-, and N-(substituted benzyl)deacetylthiocolchicines as potent cytotoxic and antimitotic compounds. |
AID115600 | MED(minimum effective dose) against P388 lymphocytic leukemia in mice; this dose produced T/C greater than the threshold value of 125 | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
| Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
AID1627657 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Chemical synthesis, pharmacological evaluation and in silico analysis of new 2,3,3a,4,5,6-hexahydrocyclopenta[c]pyrazole derivatives as potential anti-mitotic agents. |
AID42553 | Inhibits the growth of the human Burkitt lymphoma CA46 cell | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
| Antitumor agents. 172. Synthesis and biological evaluation of novel deacetamidothiocolchicin-7-ols and ester analogs as antitubulin agents. |
AID153196 | In vivo antitumor activity against P388 lymphocytic leukemia cells implanted intraperitoneally; reproducible minimal activity. | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
| Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
AID1694406 | Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
AID443470 | Cytotoxicity against human Caco-2 cells after 24 hrs by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID214171 | Effect on the binding of radiolabeled [3H]colchicine to tubulin | 1991 | Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
| Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization. |
AID1627659 | Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Chemical synthesis, pharmacological evaluation and in silico analysis of new 2,3,3a,4,5,6-hexahydrocyclopenta[c]pyrazole derivatives as potential anti-mitotic agents. |
AID139239 | Logarithm of toxic activity (1/lethal dose) in mice bearing P388 leukemia on chronic regimen (Q 1-9) | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5
| Toxicity quantitative structure--activity relationships of colchicines. |
AID1673981 | Antiproliferative activity against human TE-671 cells incubated for 36 hrs | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
AID1694414 | Cell cycle arrest in human ALL-5 cells assessed as accumulation at sub-G1 phase after 72 hrs at 5 times of IC50 by propidium iodide staining-based flow cytometric analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
AID1414056 | Antifungal activity against Chaetomium globosum BAM12 ATCC 6205 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10
| 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
AID443483 | Cytotoxicity against c-myc/c-raf double transgenic mouse betaD5 cells by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID443475 | Inhibition of microtubule in human A549 cells assessed as network disappearane at 0.5 uM after 1 hr by immunofluorescence analysis | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID514411 | Cytotoxicity against human KB cells after 2 days | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
AID213858 | Percentage by which the binding of [3H]colchicine (2.5 uM) to tubulin from calf brain is reduced by 25 uM concentration of compound | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
| A novel synthesis of colchicide and analogues from thiocolchicine and congeners: reevaluation of colchicide as a potential antitumor agent. |
AID140029 | Acute toxicity after intramuscular injection in mice. | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
| Antitubulin effects of derivatives of 3-demethylthiocolchicine, methylthio ethers of natural colchicinoids, and thioketones derived from thiocolchicine. Comparison with colchicinoids. |
AID408415 | Inhibition of pig brain tubulin polymerization assessed as ratio of unpolymerized to polymerized tubulin at 10 uM | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
| Inhibitors of tubulin polymerization: synthesis and biological evaluation of hybrids of vindoline, anhydrovinblastine and vinorelbine with thiocolchicine, podophyllotoxin and baccatin III. |
AID214375 | Inhibition of [3H]colchicine binding to microtubule protein tubulin | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
| Biological effects of modified colchicines. Improved preparation of 2-demethylcolchicine, 3-demethylcolchicine, and (+)-colchicine and reassignment of the position of the double bond in dehydro-7-deacetamidocolchicines. |
AID208873 | Cytotoxicity against human central nervous system carcinoma TE671 cell line | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic |
AID154376 | Antitumor activity against murine lymphocytic leukemia P388 cells | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
| Quantitative structure-activity relationships of colchicines against P388 leukemia in mice. |
AID214550 | Inhibition of Tubulin polymerization after 20 minutes of administration at 30 degree Centigrade | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
| Antitumor agents. 172. Synthesis and biological evaluation of novel deacetamidothiocolchicin-7-ols and ester analogs as antitubulin agents. |
AID1414049 | Antifungal activity against Aspergillus niger van Tiegen BAM4 ATCC 6275 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10
| 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
AID445541 | Cell cycle arrest in human IGROV1 cells assessed as accumulation at G2/M phase at IC80 concentration after 24 hrs using propidium iodide staining by FACS analysis relative to control | 2009 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
| Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds. |
AID492478 | Displacement of [3H]colchicine from tubulin | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3
| Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach. |
AID399881 | Inhibition of tubulin polymerization | 2004 | Journal of natural products, Feb, Volume: 67, Issue:2
| Current developments in the discovery and design of new drug candidates from plant natural product leads. |
AID443481 | Cytotoxicity against c-myc/c-raf double transgenic mouse yD1 cells by MTS assay | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID214705 | Binding affinity of [3H]- colchicine (5.0 uM) to tubulin (1.0 uM, 0.1 mg/mL) was evaluated at concentration of 5.0 uM | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
| Antitumor agents. 172. Synthesis and biological evaluation of novel deacetamidothiocolchicin-7-ols and ester analogs as antitubulin agents. |
AID1673978 | Antiproliferative activity against human A549 cells incubated for 36 hrs | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
AID3330 | In vivo antitumor activity against 3M531 is the sarcoma M5076; reproducible minimal activity | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
| Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
AID1694410 | Antiproliferative activity against mouse BALB/3T3 cells incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
AID152355 | Cytotoxicity against murine P388 leukemia cell line | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic |
AID1673961 | Inhibition of tubulin polymerization (unknown origin) | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
AID214021 | Inhibition of tubulin polymerization with preincubation for 15 minutes at 37 degree Centigrade prior to addition of the GTP required for polymerization | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic |
AID213997 | Evaluated for the inhibition of tubulin polymerization without pre-incubation | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic |
AID337171 | Antiviral activity against HIV1 HTLV-3B in human H9 cells after 3 days by p24 antigen capture assay | | | |
AID214001 | Inhibition of glutamate-dependent tubulin polymerization at 30 degrees C(0.25 mM MgCl2) | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
| Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions. |
AID1414050 | Antifungal activity against Aspergillus versicolor BAM8 ATCC 11730 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10
| 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
AID443476 | Inhibition of microtubule in human A549 cells assessed as roundish cells at 0.5 uM after 24 hrs by immunofluorescence analysis | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
| Synthesis and biological evaluation of novel thiocolchicine-podophyllotoxin conjugates. |
AID1414055 | Antifungal activity against Aureobasidium pullulans BAM10 ATCC 9348 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10
| 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
AID1809652 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Synthesis of thiocolchicine amine derivatives and evaluation of their antiproliferative activity. |
AID101630 | Anti tumor activity on human breast cancer cell line MDR-negative MDA-MB 231 after 72 hours of treatment | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25
| N-deacetyl-N-aminoacylthiocolchicine derivatives: synthesis and biological evaluation on MDR-positive and MDR-negative human cancer cell lines. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6
| A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | | | |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |