WIN 33377: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 3035776 |
| CHEMBL ID | 283395 |
| SCHEMBL ID | 676607 |
| MeSH ID | M0255008 |
| Synonym |
|---|
| CHEMBL283395 , |
| win 33377 |
| 21e5klj2zb , |
| unii-21e5klj2zb |
| sr 233377 |
| win-33377 |
| 146537-07-7 |
| sw 33377 |
| n-(((1-(2-(diethylamino)ethyl)amino)-9-oxo-9h-thioxanthen-4-yl)methyl)methanesulfonamide |
| methanesulfonamide, n-((1-((2-(diethylamino)ethyl)amino)-9-oxo-9h-thioxanthen-4-yl)methyl)- |
| win 033377 |
| SCHEMBL676607 |
| sw-33377 |
| sr-233377 |
| DTXSID30163394 |
| win33377 |
| bdbm50214148 |
| n-[[1-[2-(diethylamino)ethylamino]-9-oxothioxanthen-4-yl]methyl]methanesulfonamide |
| Q27253550 |
WIN 33377 (I) is a member of a novel class of cytotoxic antitumor agents, 4-aminomethyl thioxanthone derivatives.
| Excerpt | Reference | Relevance |
|---|---|---|
| "WIN 33377 (I) is a member of a novel class of cytotoxic antitumor agents, 4-aminomethyl thioxanthone derivatives. " | ( A column-switching high-performance liquid chromatographic assay for a novel cytotoxic thioxanthone derivative (WIN 33377) in mouse plasma with toxicokinetic results from a mouse LD10 study. Drozd, ML; Lockwood, G; Miller, B; Rosi, D, 1995) | 1.95 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The sustained high 183577 concentration in liver is believed to be responsible for its prolonged half-life and hepatotoxicity." | ( Pharmacokinetic studies in mice of two new thioxanthenones (183577 and 232759) that showed preferential solid tumor activity. Corbett, TH; Foster, BJ; LoRusso, PM; Pugh, S; Rake, J; Wiegand, RA, 1997) | 0.3 |
| " Pharmacokinetic sampling was performed during the first cycle in all patients." | ( Phase I/pharmacokinetic trial of the novel thioxanthone SR233377 (WIN33377) on a 5-day schedule. DeMaria, D; Drozd, M; Graham, MA; Lockwood, G; O'Dwyer, PJ; Purvis, JD; Reilly, D; Stevenson, JP, 1999) | 0.3 |
| " SR233377 Cmax values increased linearly with dose, but substantial interpatient variability in SR233377 AUC, clearance, and half-life was noted." | ( Phase I/pharmacokinetic trial of the novel thioxanthone SR233377 (WIN33377) on a 5-day schedule. DeMaria, D; Drozd, M; Graham, MA; Lockwood, G; O'Dwyer, PJ; Purvis, JD; Reilly, D; Stevenson, JP, 1999) | 0.3 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " The utility of the method was demonstrated by analyzing plasma samples obtained from mice dosed with I as part of a pre-clinical safety study intended to assist in the design of a pharmacokinetically guided dose escalation strategy." | ( A column-switching high-performance liquid chromatographic assay for a novel cytotoxic thioxanthone derivative (WIN 33377) in mouse plasma with toxicokinetic results from a mouse LD10 study. Drozd, ML; Lockwood, G; Miller, B; Rosi, D, 1995) | 0.5 |
| "We conclude that SR233377 administered on a 5-day schedule is associated with tolerable clinical symptoms and some activity against a range of solid tumors but dosing is limited by QTc prolongation, a condition that predisposes to ventricular arrhythmias." | ( Phase I/pharmacokinetic trial of the novel thioxanthone SR233377 (WIN33377) on a 5-day schedule. DeMaria, D; Drozd, M; Graham, MA; Lockwood, G; O'Dwyer, PJ; Purvis, JD; Reilly, D; Stevenson, JP, 1999) | 0.3 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| DNA topoisomerase 2-alpha | Homo sapiens (human) | EC50 (µMol) | 3.0000 | 0.7200 | 1.2900 | 3.0000 | AID211289 |
| DNA topoisomerase 2-beta | Homo sapiens (human) | EC50 (µMol) | 3.0000 | 0.7200 | 1.2900 | 3.0000 | AID211289 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID137218 | In vivo antitumor activity measured in mice against the Panc 02 murine solid tumors. | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives. |
| AID134904 | The long term cures (LTC) value is the number of mice in a group with no palpable tumor. | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives. |
| AID134219 | The log cell kill of tumor-bearing mice, based on tumor growth delay. | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives. |
| AID136057 | Compound was tested for in vivo growth inhibition of pancreatic ductal adenocarcinoma (Panc 03) in mice, expressed as antitumor efficacy; description for activity not available | 1994 | Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6 | Comparative molecular field analysis of the antitumor activity of 9H-thioxanthen-9-one derivatives against pancreatic ductal carcinoma 03. |
| AID137214 | In vivo antitumor activity measured in mice against the Colon26/A murine solid tumors. | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives. |
| AID211289 | In vitro evaluation for inhibitor of human topoisomerase II from HeLa cells. | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives. |
| AID136055 | In vivo antitumor activity in mice implanted with murine pancreatic adenocarcinoma 03, T/C value (total/control) | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives. |
| AID137217 | In vivo antitumor activity measured in mice against the Mam16/C murine solid tumors. | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives. |
| AID150540 | In vitro cytotoxicity measured by quantifying clonogenic survival in soft agar following a 1-hour transient exposure of p388 mouse leukemia cells. | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives. |
| AID46155 | In vitro evaluation for intercalating potency by using calf thymus DNA in ethidium bromide displacement assay | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives. |
| AID133779 | Maximum tolerated dose administarted iv (mg/kg) to mice | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives. |
| AID137215 | In vivo antitumor activity measured in mice against the Colon38 murine solid tumors. | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives. |
| AID137216 | In vivo antitumor activity measured in mice against the Colon51 murine solid tumors. | 1998 | Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19 | Synthesis and antitumor activity of 4-aminomethylthioxanthenone and 5-aminomethylbenzothiopyranoindazole derivatives. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 5 (71.43) | 18.2507 |
| 2000's | 2 (28.57) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (11.78) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (25.00%) | 5.53% |
| Reviews | 1 (12.50%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (62.50%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||