Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C22H28N4O4 |
| Molecular Weight | 412.4821 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OCCNCCNC1=CC=C(NCCNCCO)C2=C1C(=O)C3=C(C=CC=C3)C2=O
InChI
InChIKey=FFGSXKJJVBXWCY-UHFFFAOYSA-N
InChI=1S/C22H28N4O4/c27-13-11-23-7-9-25-17-5-6-18(26-10-8-24-12-14-28)20-19(17)21(29)15-3-1-2-4-16(15)22(20)30/h1-6,23-28H,7-14H2
Ametantrone (AM) is a synthetic 9,10-anthracenedione bearing two (hydroxyethylamino)ethylamino residues at positions 1 and 4; along with other anthraquinones and anthracyclines, it shares a polycyclic intercalating moiety and charged side chains that stabilize DNA binding. Ametantrone is anticancer drug candidate targeting DNA. Ametantrone is a topoisomerase II inhibitor of the anthrapyrazole family. Ametantrone induces interstrand DNA cross-links in HeLa S3 cells. These cross-links were observed only in cellular system suggesting that metabolism of the drugs is a necessary step leading to DNA cross-linking. Ametantrone appeared to be very well tolerated and easy to handle. A dose-schedule of 135 mg/m2 q 2–3 weeks was recommended for phase II studies in solid tumors.
Approval Year
Sample Use Guides
Sixteen patients received 33 courses of drug as a single iv dose given every 3 weeks. Escalations proceeded from 120 to 180 mg/m2. A dose of 140-160 mg/m2 is recommended as the starting dose for phase II trials in patients who have received prior chemotherapy or radiotherapy.
Route of Administration:
Intravenous
84 of 228 tumors plated for the ametantrone study were evaluable for drug-sensitivity assays. The overall in vitro response rates (defined as a less than or equal to 50% survival of tumor colony-forming units) for ametantrone were 13%, 21%, and 26% at 0.1, 1, and 10 ug/ml, respectively.
| Name | Type | Language | ||
|---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Code | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
NCI_THESAURUS |
C253
Created by
admin on Fri Dec 15 16:02:25 GMT 2023 , Edited by admin on Fri Dec 15 16:02:25 GMT 2023
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
100000087214
Created by
admin on Fri Dec 15 16:02:25 GMT 2023 , Edited by admin on Fri Dec 15 16:02:25 GMT 2023
|
PRIMARY | |||
|
SUB05410MIG
Created by
admin on Fri Dec 15 16:02:25 GMT 2023 , Edited by admin on Fri Dec 15 16:02:25 GMT 2023
|
PRIMARY | |||
|
5023
Created by
admin on Fri Dec 15 16:02:25 GMT 2023 , Edited by admin on Fri Dec 15 16:02:25 GMT 2023
|
PRIMARY | |||
|
PNT6041ST1
Created by
admin on Fri Dec 15 16:02:25 GMT 2023 , Edited by admin on Fri Dec 15 16:02:25 GMT 2023
|
PRIMARY | |||
|
2134
Created by
admin on Fri Dec 15 16:02:25 GMT 2023 , Edited by admin on Fri Dec 15 16:02:25 GMT 2023
|
PRIMARY | |||
|
CHEMBL49442
Created by
admin on Fri Dec 15 16:02:25 GMT 2023 , Edited by admin on Fri Dec 15 16:02:25 GMT 2023
|
PRIMARY | |||
|
196473
Created by
admin on Fri Dec 15 16:02:25 GMT 2023 , Edited by admin on Fri Dec 15 16:02:25 GMT 2023
|
PRIMARY | |||
|
C1342
Created by
admin on Fri Dec 15 16:02:25 GMT 2023 , Edited by admin on Fri Dec 15 16:02:25 GMT 2023
|
PRIMARY | |||
|
C020182
Created by
admin on Fri Dec 15 16:02:25 GMT 2023 , Edited by admin on Fri Dec 15 16:02:25 GMT 2023
|
PRIMARY | |||
|
DTXSID60215153
Created by
admin on Fri Dec 15 16:02:25 GMT 2023 , Edited by admin on Fri Dec 15 16:02:25 GMT 2023
|
PRIMARY | |||
|
64862-96-0
Created by
admin on Fri Dec 15 16:02:25 GMT 2023 , Edited by admin on Fri Dec 15 16:02:25 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
SALT/SOLVATE (PARENT)
