Ferreira, Ricardo J.; Gajdacs, Mario; Kincses, Annamaria; Spengler, Gabriella; dos Santos, Daniel J. V. A.; Ferreira, Maria-Jose U. published the article 《Nitrogen-containing naringenin derivatives for reversing multidrug resistance in cancer》. Keywords: preparation nitrogen containing naringenin derivative reversing multidrug resistance cancer; Docking; Efflux modulators; Flavonoids; Molecular dynamics; Multidrug resistance; P-glycoprotein.They researched the compound: 2-Furoic hydrazide( cas:3326-71-4 ).Application of 3326-71-4. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:3326-71-4) here.
Naringenin (1), isolated from Euphorbia pedroi, was previously derivatized yielding compounds 2-13. In this study, aiming at expanding the pool of analogs of the flavanone core towards better multidrug resistance (MDR) reversal agents, alkylation reactions and chem. modification of the carbonyl moiety was performed (15-39). Compounds structures were assigned mainly by 1D and 2D NMR experiments Compounds 1-39 were assessed as MDR reversers, in human ABCB1-transfected mouse T-lymphoma cells, overexpressing P-glycoprotein (P-gp). The results revealed that O-methylation at C-7, together with the introduction of nitrogen atoms and aromatic moieties at C-4 or C-4′, significantly improved the activity, being compounds 27 and 37 the strongest P-gp modulators and much more active than verapamil. In combination assays, synergistic interactions of selected compounds with doxorubicin substantiated the results. While mol. docking suggested that flavanone derivatives act as competitive modulators, mol. dynamics showed that dimethylation promotes binding to a modulator-binding site. Moreover, flavanones may also interact with a vicinal ATP-binding site in both nucleotide-binding domains, hypothesizing an allosteric mode of action.
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Reference:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics