diacetyldiphenylurea bisguanylhydrazone: antineoplastic agent particularly effective as an antileukemic agent; has been shown to be active against leukemia L1210 in mice; minor descriptor (75-86); on-line & INDEX MEDICUS search CARBANILIDES (75-86); RN given refers to parent cpd [MeSH]
| ID Source | ID |
|---|---|
| PubMed CID | 6328182 |
| CHEMBL ID | 142485 |
| SCHEMBL ID | 13431057 |
| MeSH ID | M0263235 |
| Synonym |
|---|
| ddug |
| brn 2793715 |
| urea, 1,3-bis(p-acetylphenyl)-, bisamidinohydrazone |
| 1,3-bis(p-acetylphenyl)urea bisamidinohydrazone |
| 4,4'-diacetylcarbanilide 4,4'-bis(amidinohydrazone) |
| diacetyldiphenylurea bisguanylhydrazone |
| carbanilide, 4,4'-diacetyl-, 4,4'-bis(aminohydrazone) |
| 4,4'-diacetyldiphenylurea-bis-(guanylhydrazone) |
| hydrazinecarboximidamide, 2,2'-(carbonylbis(imino-4,1-phenyleneethylidyne)bis- |
| CHEMBL142485 |
| bdbm34063 |
| 1,3-bis[4-[(e)-n-(diaminomethylideneamino)-c-methylcarbonimidoyl]phenyl]urea |
| 13284-07-6 |
| hydrazinecarboximidamide, 2,2'-(carbonylbis(imino-4,1-phenyleneethylidyne))bis- |
| SCHEMBL13431057 |
| 4,4'-diacetyldiphenylurea-bis(guanylhydrazone) |
| (2e)-2-(1-{4-[({4-[(1e)-n-carbamimidoylethanehydrazonoyl]phenyl}carbamoyl)amino]phenyl}ethylidene)hydrazinecarboximidamide (non-preferred name) |
| 1048364-29-9 |
| NCGC00487389-01 |
| (2e,2'e)-2,2'-(((carbonylbis(azanediyl))bis(4,1-phenylene))bis(ethan-1-yl-1-ylidene))bis(hydrazinecarboximidamide) |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| Serine/threonine-protein kinase Chk2 | Homo sapiens (human) | IC50 | 0.2200 | AID1799260; AID1799261 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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 ISSN: 1521-0111 | 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 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1130855 | Displacement of ethidium from poly[d(A-T)]-poly[d(A-T)] DNA (unknown origin) by fluorimetric assay | 1979 | Journal of medicinal chemistry, Oct, Volume: 22, Issue:10 ISSN: 0022-2623 | Potential antitumor agents. 31. Quantitative structure-activity relationships for the antileukemic bis(guanylhydrazones). |
| AID1130856 | Displacement of ethidium from poly[d(G-C)]-poly[d(G-C)] DNA (unknown origin) by fluorimetric assay | 1979 | Journal of medicinal chemistry, Oct, Volume: 22, Issue:10 ISSN: 0022-2623 | Potential antitumor agents. 31. Quantitative structure-activity relationships for the antileukemic bis(guanylhydrazones). |
| AID1130853 | Anti-leukemic activity against mouse L1210 cells allografted in ip dosed DBA2 mouse assessed as optimum drug dose required for the effect administered qd for 1 to 4 days | 1979 | Journal of medicinal chemistry, Oct, Volume: 22, Issue:10 ISSN: 0022-2623 | Potential antitumor agents. 31. Quantitative structure-activity relationships for the antileukemic bis(guanylhydrazones). |
| AID1130854 | Binding affinity to DNA (unknown origin) assessed as decrease in velocity of L1210 DNA-dependent DNA polymerase reaction | 1979 | Journal of medicinal chemistry, Oct, Volume: 22, Issue:10 ISSN: 0022-2623 | Potential antitumor agents. 31. Quantitative structure-activity relationships for the antileukemic bis(guanylhydrazones). |
| AID341692 | Therapeutic index, ratio of CC50 for BHK15 cells to EC50 IRES-luciferase tagged Yellow fever virus | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 ISSN: 1520-4804 | Design, synthesis, and biological evaluation of antiviral agents targeting flavivirus envelope proteins. |
| AID1130852 | Anti-leukemic activity against mouse L1210 cells allografted in ip dosed DBA2 mouse assessed as increase in host lifespan administered qd for 1 to 4 days | 1979 | Journal of medicinal chemistry, Oct, Volume: 22, Issue:10 ISSN: 0022-2623 | Potential antitumor agents. 31. Quantitative structure-activity relationships for the antileukemic bis(guanylhydrazones). |
| AID341691 | Cytotoxicity against BHK15 cells assessed as cell viability after 36 hrs by MTT assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 ISSN: 1520-4804 | Design, synthesis, and biological evaluation of antiviral agents targeting flavivirus envelope proteins. |
| AID341690 | Antiviral activity against IRES-luciferase tagged Yellow fever virus in BHK15 cells assessed as reduction of luciferase activity after 36 hrs | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 ISSN: 1520-4804 | Design, synthesis, and biological evaluation of antiviral agents targeting flavivirus envelope proteins. |
| AID26757 | DNA binding dissociation constant as KD; No data | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 ISSN: 0022-2623 | Interactions of antitumor drugs with natural DNA: 1H NMR study of binding mode and kinetics. |
| AID1799260 | In Vitro Protein Kinase Assay from Article 10.1124/mol.107.035832: \\Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase.\\ | 2007 | Molecular pharmacology, Oct, Volume: 72, Issue:4 ISSN: 0026-895X | Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase. |
| AID1799261 | IMAP High-Throughput Screening from Article 10.1124/mol.107.035832: \\Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase.\\ | 2007 | Molecular pharmacology, Oct, Volume: 72, Issue:4 ISSN: 0026-895X | Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 7 (58.33) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (25.00) | 29.6817 |
| 2010's | 2 (16.67) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 12 (100.00%) | 84.16% |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Angioblastic Meningioma | 0 | 2011 | 2011 | 13.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 | |
| Experimental Hepatoma | 0 | 1983 | 1983 | 41.0 | medium | 0 | 1 | 0 | 0 | 0 | 0 | |
| Leukemia L 1210 | 0 | 1979 | 1987 | 41.8 | high | 0 | 5 | 0 | 0 | 0 | 0 | |
| Meningioma | 0 | 2011 | 2011 | 13.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| Article | Year |
|---|---|
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular pharmacology, , Volume: 96, Issue:5 | 2019 |