Page last updated: 2024-11-12
doxazolidine
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Description
doxazolidine: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 11599300 |
| CHEMBL ID | 217089 |
| SCHEMBL ID | 12567109 |
| MeSH ID | M0542203 |
Synonyms (4)
| Synonym |
|---|
| doxazolidine |
| CHEMBL217089 |
| SCHEMBL12567109 |
| (7s,9s)-7-[[(3as,4s,6r,7as)-4-methyl-2,3a,4,6,7,7a-hexahydro-1h-pyrano[4,3-d][1,3]oxazol-6-yl]oxy]-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7h-tetracene-5,12-dione |
Research Excerpts
Overview
Doxazolidine (doxaz) is a new anthracycline anticancer agent. It induces cancer cell death in Dox-sensitive and resistant cells.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Doxazolidine (Doxaz) is a functionally distinct formaldehyde conjugate of doxorubicin (Dox) that induces cancer cell death in Dox-sensitive and resistant cells. " | ( Preclinical efficacy of a carboxylesterase 2-activated prodrug of doxazolidine. Barthel, BL; Chan, DC; Coldren, CD; Koch, GG; Koch, TH; Polinkovsky, M; Rudnicki, DL; Sun, H; Zhang, Z, 2009) | 2.03 |
| "Doxazolidine (doxaz) is a new anthracycline anticancer agent. " | ( Synthesis and biological characterization of protease-activated prodrugs of doxazolidine. Barthel, BL; Burkhart, DJ; Colvin, SM; Kirby, TP; Koch, TH; Rudnicki, DL, 2012) | 2.05 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| "The results in this study suggest that FOLFIRI, a common regimen combining irinotecan and 5-FU, should switch the dosing sequence, namely from 5-FU to irinotecan, to enhance hydrolytic activation of irinotecan." | ( Regulation of carboxylesterase-2 expression by p53 family proteins and enhanced anti-cancer activities among 5-fluorouracil, irinotecan and doxazolidine prodrug. Charpentier, M; Guo, L; Lu, W; Xiao, D; Yan, B; Yang, D, 2013) | 0.59 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Bioassays (29)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID297711 | Growth inhibition of human RXF393 cells after 48 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297705 | Growth inhibition of human HL60(TB) cells after 48 hrs by crystal violet assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297722 | Induction of apoptosis in HL60 cells assessed as annexin V positive cells | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID272794 | Growth inhibition of HepG2 cells by crystal violet assay after 3 hrs | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Design, synthesis, and preliminary evaluation of doxazolidine carbamates as prodrugs activated by carboxylesterases. |
| AID272789 | Growth inhibition of MCF7/Adr cells by crystal violet assay after 3 hrs | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Design, synthesis, and preliminary evaluation of doxazolidine carbamates as prodrugs activated by carboxylesterases. |
| AID297699 | Growth inhibition of human SHP77 cells after 3 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID272796 | Growth inhibition of rat H9c2(2-1) cells by MTT assay after 3 hrs | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Design, synthesis, and preliminary evaluation of doxazolidine carbamates as prodrugs activated by carboxylesterases. |
| AID272798 | Cytotoxicity against Vero cells by MTT assay after 3 hrs | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Design, synthesis, and preliminary evaluation of doxazolidine carbamates as prodrugs activated by carboxylesterases. |
| AID297707 | Growth inhibition of human HCT116 cells after 48 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID468900 | Toxicity in athymic nude mouse xenografted with human NCI-H1435 cells expressing CES2 gene assessed as lipid peroxidation in hepatocytes administered with six iv injection of 3 to 4 mg/kg by hematoxylin/eosin staining-based microscopy | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Preclinical efficacy of a carboxylesterase 2-activated prodrug of doxazolidine. |
| AID297701 | Growth inhibition of human PC3 cells after 3 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID272792 | Growth inhibition of SK-HEP-1 cells by crystal violet assay after 3 hrs | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Design, synthesis, and preliminary evaluation of doxazolidine carbamates as prodrugs activated by carboxylesterases. |
| AID297710 | Growth inhibition of human IGROVI cells after 48 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297721 | Induction of apoptosis in human HCT116 cells at 200 nM for 3 hrs by annexin V staining assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297712 | Growth inhibition of human DU145 cells after 48 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297706 | Growth inhibition of human NCIH460 cells after 48 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297717 | Effect on G2/M arrest in topoisomerase 2 deficient human HL60/MX2 cells at 100 nM after 24 hrs | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297720 | Induction of apoptosis in human HCT116 cells at 50 nM for 3 hrs by annexin V staining assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297704 | Growth inhibition of human BxPc3 cells after 3 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID272799 | Cytotoxicity against Vero cells by MTT assay after 24 hrs | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Design, synthesis, and preliminary evaluation of doxazolidine carbamates as prodrugs activated by carboxylesterases. |
| AID297708 | Growth inhibition of human SF268 cells after 48 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297723 | Induction of apoptosis in topoisomerase 2 deficient HL60/MX2 cells assessed as annexin V positive cells | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID272788 | Growth inhibition of MCF7 cells by crystal violet assay after 3 hrs | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Design, synthesis, and preliminary evaluation of doxazolidine carbamates as prodrugs activated by carboxylesterases. |
| AID297715 | Induction of apoptosis in human HCT116 cells at 400 nM for 3 hrs relative to control cells by annexin V staining assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297719 | Inhibition of topoisomerase 2 at 50 nM by decatenation assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297702 | Growth inhibition of human MDA-MB-435 cells after 3 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297709 | Growth inhibition of human UACC257 cells after 48 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297703 | Growth inhibition of human MiaPaCa2 cells after 3 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| AID297700 | Growth inhibition of human A375 cells after 3 hrs by MTT assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (12)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (33.33) | 29.6817 |
| 2010's | 7 (58.33) | 24.3611 |
| 2020's | 1 (8.33) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Study Types
| 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% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||