Journal
FUTURE MEDICINAL CHEMISTRY
Volume 10, Issue 7, Pages 725-741Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2017-0228
Keywords
ABC transporters; BCRP; flavanone; hydrazides; hydrazones; molecular docking; MRP1; multidrug resistance; P-gp; pharmacophore
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Funding
- European Structural & Investment Funds through the COMPETE Programme
- FCT - Fundacao para a Ciencia e a Tecnologia (FCT) [PTDC/QEQ-MED/0905/2012, UID/DTP/04138/2013, SAICTPAC/0019/2015]
- FCT [SFRH/BD/84285/2012]
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Aim: Naringenin (1), isolated in large amount from the aerial parts of Euphorbia pedroi, was chemically derivatized to yield 18 imine derivatives (2-19) and three alkylated derivatives through a Mannich-type reaction (20-22) that were tested as multidrug resistance (MDR) reversers in cancer cells. Results/methodology: While hydrazone (2-4) and azine (5-13) derivatives showed an improvement in their MDR reversal activities against the breast cancer resistance protein, carbohydrazides 14-19 revealed an enhancement in MDR reversal activity toward the multidrug resistance protein 1. Conclusion: The observed activities, together with pharmacophoric analysis and molecular docking studies, identified the spatial orientation of the substituents as a key structural feature toward a possible mechanism by which naringenin derivatives may reverse MDR in cancer.
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