Flavonoid derivatives as selective ABCC1 modulators: Synthesis and functional characterization was written by Obreque-Balboa, Jose Esteban;Sun, Qiu;Bernhardt, Guenther;Koenig, Burkhard;Buschauer, Armin. And the article was included in European Journal of Medicinal Chemistry in 2016.Recommanded Product: 72141-41-4 This article mentions the following:
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: ABCC1, IC50 11.3 μM; inactive at ABCB1 and ABCG2). This compound 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 2-[4-(Benzo[c][1,2,5]oxadiazol-5-ylmethyl)piperazin-1-yl]-5,7-dimethoxy-4H-chromen-4-one, were of potential value as pharmacol. tools for the investigation of the (patho)physiol. role of ABCC1. In the experiment, the researchers used many compounds, for example, (4-Nitrophenyl)(piperazin-1-yl)methanone (cas: 72141-41-4Recommanded Product: 72141-41-4).
(4-Nitrophenyl)(piperazin-1-yl)methanone (cas: 72141-41-4) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Recommanded Product: 72141-41-4
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics