91098-69-0Relevant articles and documents
Flavonoid derivatives as selective ABCC1 modulators: Synthesis and functional characterization
Obreque-Balboa, José Esteban,Sun, Qiu,Bernhardt, Günther,K?nig, Burkhard,Buschauer, Armin
supporting information, p. 124 - 133 (2016/01/20)
A series of chromones, bearing substituted amino groups or N-substituted carboxamide moieties in position 2, was synthesized and characterized in cellular assays for modulation of the ABC transporters ABCC1 (MDCKII-MRP1 cells), ABCB1 (Kb-V1 cells) and ABCG2 (MCF-7/Topo cells). The most potent ABCC1 modulators identified among these flavonoid-type compounds were comparable to the reference compound reversan regarding potency, but superior in terms of selectivity concerning ABCB1 and ABCG2 (2-[4-(Benzo[c][1,2,5]oxadiazol-5-ylmethyl)piperazin-1-yl]-5,7-dimethoxy-4H-chromen-4-one (51): ABCC1, IC50 11.3-1/4M; inactive at ABCB1 and ABCG2). Compound 51 was as effective as reversan in reverting ABCC1-mediated resistance to cytostatics in MDCKII-MRP1 cells and proved to be stable in mouse plasma and cell culture medium. Modulators, such as compound 51, are of potential value as pharmacological tools for the investigation of the (patho)physiological role of ABCC1.
Synthesis and class III type antiarrhythmic activity of 4-Aroyl (and Aryl)-1-aralkylpiperazines
Kanojia, Ramesh M.,Salata, Joseph J.,Kauffman, Jack
, p. 2819 - 2823 (2007/10/03)
The synthesis and in vitro Class III antiarrhythmic activity of several 4-aroyl (and aryl)-1-aralkylpiperazine and piperidine derivatives are described. Among several potent compounds identified in the series, RWJ-28810 (3), with its EC20 of 3 nM, ranks as one of the most potent (in vitro) compounds reported. (C) 2000 Elsevier Science Ltd.