Flavonoid Oxime Carbamate Derivatives Reversal of Multidrug Resistance in Cancer Cells /
The effectiveness of cancer treatment has been seriously hindered by the development of multidrug resistance (MDR), mainly mediated by efflux transporters such as P‐glycoprotein (P‐gp/ABCB1). Aiming at obtaining new compounds for overcoming MDR in cancer, tangeretin ( 1 ), a natural polymethoxyflavo...
Elmentve itt :
| Szerzők: | |
|---|---|
| Dokumentumtípus: | Cikk |
| Megjelent: |
2026
|
| Sorozat: | CHEMMEDCHEM
21 No. 7 |
| Tárgyszavak: | |
| doi: | 10.1002/cmdc.202501113 |
| mtmt: | 37093174 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/40008 |
| LEADER | 02351nab a2200289 i 4500 | ||
|---|---|---|---|
| 001 | publ40008 | ||
| 005 | 20260430103858.0 | ||
| 008 | 260430s2026 hu o 000 eng d | ||
| 022 | |a 1860-7179 | ||
| 024 | 7 | |a 10.1002/cmdc.202501113 |2 doi | |
| 024 | 7 | |a 37093174 |2 mtmt | |
| 040 | |a SZTE Publicatio Repozitórium |b hun | ||
| 041 | |a eng | ||
| 100 | 1 | |a Barbosa Filipa | |
| 245 | 1 | 0 | |a Flavonoid Oxime Carbamate Derivatives |h [elektronikus dokumentum] : |b Reversal of Multidrug Resistance in Cancer Cells / |c Barbosa Filipa |
| 260 | |c 2026 | ||
| 300 | |a 14 | ||
| 490 | 0 | |a CHEMMEDCHEM |v 21 No. 7 | |
| 520 | 3 | |a The effectiveness of cancer treatment has been seriously hindered by the development of multidrug resistance (MDR), mainly mediated by efflux transporters such as P‐glycoprotein (P‐gp/ABCB1). Aiming at obtaining new compounds for overcoming MDR in cancer, tangeretin ( 1 ), a natural polymethoxyflavonoid, was derivatized. After obtaining the corresponding oxime ( 2 ), a set of 23 novel oxime carbamates ( 3 – 26 ) was prepared via carbonyldiimidazole‐mediated reaction with various amines or by reaction with isocyanates. Their structures were assigned mainly by 1D and 2D NMR experiments. The compounds ( 1–26 ) were evaluated for their MDR reversal potential, using the rhodamine‐123 accumulation assay and chemosensitivity experiments, in human ABCB1 ‐gene transfected L5178Y mouse lymphoma cells. A significant increase in P‐gp inhibitory activity was observed for most of the derivatives at noncytotoxic concentrations. Notably, compounds 19 , 20 , and 22 , bearing an aliphatic substituent, were the most active, exhibiting a strong MDR reversal effect at 2 μM. Moreover, drug combination assays revealed that most of the derivatives were able to synergize doxorubicin. Selected compounds were also tested in the ATPase assay, where most of them acted as inhibitors. | |
| 650 | 4 | |a Biológiai tudományok | |
| 650 | 4 | |a Általános orvostudomány | |
| 700 | 0 | 1 | |a Spengler Gabriella |e aut |
| 700 | 0 | 1 | |a Bózsity Noémi |e aut |
| 700 | 0 | 1 | |a Szemerédi Nikoletta |e aut |
| 700 | 0 | 1 | |a Zupkó István |e aut |
| 700 | 0 | 1 | |a Ferreira Maria‐José U. |e aut |
| 856 | 4 | 0 | |u http://publicatio.bibl.u-szeged.hu/40008/1/Spengler_ChemMedChem-2026-Barbosa-FlavonoidOximeCarbamateDerivativesReversalofMultidrugResistanceinCancerCells.pdf |z Dokumentum-elérés |