So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Dhainaut, Alain; Regnier, Gilbert; Atassi, Ghanem; Pierre, Alain; Leonce, Stephane; Kraus-Berthier, Laurence; Prost, Jean Francois researched the compound: 1-(Bis(4-chlorophenyl)methyl)piperazine( cas:27469-61-0 ).Recommanded Product: 27469-61-0.They published the article 《New triazine derivatives as potent modulators of multidrug resistance》 about this compound( cas:27469-61-0 ) in Journal of Medicinal Chemistry. Keywords: triazine modulator multidrug resistance; cytotoxic agent modulator multidrug resistance triazine; structure activity multidrug resistance modulator triazine. We’ll tell you more about this compound (cas:27469-61-0).
70 Triazines, e.g., I (X = bond, NH, aminoalkylene; Y = N; R = diarylalkyl, dibenzocycloheptenyl, dibenzoheteroaryl) were prepared from chlorotrazines and tested for their capacity to modulate multidrug resistance (MDR) in DC-3F/AD and KB-A1 tumor cells in vitro, in comparison with verapamil (VRP), a calcium channel antagonist currently used in therapy as an antihypertensive drug, which also shows MDR modulating activity. Among the 12 selected compounds, I [X = bond, Y = CH, R = NHCH2CH(C6H4F-4)2] (II) (S9788) showed high MDR reversing properties in vitro (300- and 6-fold VRP at 5 μM in DC-3F/AD and KB-A1 cells, resp.) and induced a strong accumulation of adriamycin. The relationship between the increase of ADR accumulation and the fold reversal induced by these compounds and their lack of effects on the sensitive DC-3F cells suggest that they act mainly by inhibiting the Pgp-catalyzed efflux of cytotoxic agents, as already described for a majority of MDR modulators. In vivo, in association with the antitumor drug vincristine (0.25 mg/kg), II (100 mg/kg) increased the T/C by 39% in mice bearing the resistant tumor cell line P388/VCR. According to these interesting properties, II was selected for a clin. development because it was more bioavailable than I [X = bond, Y = CH, R = (dibenzo[a,d]cyclohepten-5-ylmethyl)amino] , even though it was less active.
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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics