2-methoxyoestra-1,3,5(10),16-tetraene-3-carboxamide: antineoplastic agent and tubulin modulator; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 11483754 |
| CHEMBL ID | 1080759 |
| SCHEMBL ID | 2112544 |
| MeSH ID | M0523260 |
| Synonym |
|---|
| irc-110160 |
| 2-methoxyoestra-1,3,5(10),16-tetraene-3-carboxamide |
| enmd-1198 |
| CHEMBL1080759 |
| 864668-87-1 |
| unii-760o4gjb9o |
| enmd 1198 |
| irc 110160 |
| 760o4gjb9o , |
| 2-methoxyestra-1(10),2,4,16-tetraene-3-carboxamide |
| estra-1(10),2,4,16-tetraene-3-carboxamide, 2-methoxy- |
| DTXSID40235571 |
| SCHEMBL2112544 |
| HY-16196 |
| CS-6766 |
| (8s,9s,13r,14s)-2-methoxy-13-methyl-6,7,8,9,11,12,14,15-octahydrocyclopenta[a]phenanthrene-3-carboxamide |
| DB05959 |
| enmd-119 |
| (13r)-2-methoxy-13-methyl-6,7,8,9,11,12,14,15-octahydrocyclopenta[a]phenanthrene-3-carboxamide |
| Q27266427 |
| MS-24541 |
| AKOS040741708 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The most active analogs were evaluated for iv and oral pharmacokinetic properties via cassette dosing in rat and in mice pharmacokinetic models." | ( Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol. Agoston, GE; Hanson, AD; LaVallee, TM; Pribluda, V; Shah, JH; Suwandi, L; Treston, AM; Zhan, X, 2009) | 0.35 |
| "ENMD-1198 is well-tolerated with a pharmacokinetic exposure profile compatible with once daily dosing." | ( A phase I dose-escalation, safety and pharmacokinetic study of the 2-methoxyestradiol analog ENMD-1198 administered orally to patients with advanced cancer. Camidge, DR; Diab, S; Eckhardt, SG; Gore, L; Gustafson, D; Leong, S; Lewis, K; Messersmith, WA; Nallapareddy, S; Sidor, C; Treston, AM; Zhou, Q, 2011) | 0.37 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " These studies highlight the activity of two orally bioavailable anti-cancer agents one of which, STX140, may offer a significant clinical advantage over existing drugs as a common dose limiting factor, haemotoxicity, may be minimised." | ( A comparison of two orally bioavailable anti-cancer agents, IRC-110160 and STX140. Ali, T; Foster, PA; Leese, MP; Newman, SP; Potter, BV; Purohit, A; Reed, MJ; Stengel, C, ) | 0.37 |
| " ENMD-1198 is an analog of 2ME2 which was developed to decrease the metabolism and increase both the bioavailability and antitumor activities of the parent molecule." | ( A phase I dose-escalation, safety and pharmacokinetic study of the 2-methoxyestradiol analog ENMD-1198 administered orally to patients with advanced cancer. Camidge, DR; Diab, S; Eckhardt, SG; Gore, L; Gustafson, D; Leong, S; Lewis, K; Messersmith, WA; Nallapareddy, S; Sidor, C; Treston, AM; Zhou, Q, 2011) | 0.37 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " The most active analogs were evaluated for iv and oral pharmacokinetic properties via cassette dosing in rat and in mice pharmacokinetic models." | ( Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol. Agoston, GE; Hanson, AD; LaVallee, TM; Pribluda, V; Shah, JH; Suwandi, L; Treston, AM; Zhan, X, 2009) | 0.35 |
| " Cycle 1 consisted of 28 days daily dosing followed by a 14-(Part A) or 7-(Part B) day observation period, then continuously in 28 day cycles thereafter." | ( A phase I dose-escalation, safety and pharmacokinetic study of the 2-methoxyestradiol analog ENMD-1198 administered orally to patients with advanced cancer. Camidge, DR; Diab, S; Eckhardt, SG; Gore, L; Gustafson, D; Leong, S; Lewis, K; Messersmith, WA; Nallapareddy, S; Sidor, C; Treston, AM; Zhou, Q, 2011) | 0.37 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID469621 | AUC (0 to infinity) in CD1 mouse at 45 mg/m'2 of body surface, po administered as single dose | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol. |
| AID469629 | Antiproliferative activity against human MCF7 cells after 48 hrs by WST1 assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol. |
| AID469627 | Ratio of 2ME2 IC50 to compound IC50 for antiangiogenic activity against HUVEC | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol. |
| AID469618 | Cmax in CD1 mouse at 45 mg/m'2 of body surface, po administered as single dose | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol. |
| AID469620 | Half life in CD1 mouse at 45 mg/m'2 of body surface, po administered as single dose | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol. |
| AID469619 | Ratio of compound Cmax to 2ME2 Cmax in CD1 mouse at 45 mg/m'2 of body surface, po administered as single dose | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol. |
| AID469625 | Ratio of 2ME2 IC50 to compound IC50 for human MDA-MB-231 cells | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol. |
| AID469623 | Antiangiogenic activity against HUVEC assessed as growth inhibition after 48 hrs by WST1 assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol. |
| AID469628 | Ratio of compound AUC (0 to infinity) to 2ME2 AUC (0 to infinity) in CD1 mouse at 45 mg/m'2 of body surface, po administered as single dose | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol. |
| AID469622 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by WST1 assay | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis, antiproliferative, and pharmacokinetic properties of 3- and 17-double-modified analogs of 2-methoxyestradiol. |
| [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 | 0 (0.00) | 18.2507 |
| 2000's | 3 (42.86) | 29.6817 |
| 2010's | 4 (57.14) | 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 (12.14) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (12.50%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (87.50%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||