《Anticancer potential of new 3-nitroaryl-6-(N-methyl)piperazin-1,2,4-triazolo[3,4-a]phthalazines targeting voltage-gated K+ channel: Copper-catalyzed one-pot synthesis from 4-chloro-1-phthalazinyl-arylhydrazones》 was written by Romero, Angel H.; Sojo, Felipe; Arvelo, Francisco; Calderon, Christian; Morales, Alvaro; Lopez, Simon E.. Recommanded Product: 1-MethylpiperazineThis research focused ontriazolophthalazine preparation anticancer mol docking potassium channel; 1,2,4-triazolo-phthalazine; Anticancer activity; CH oxidative cyclization; Molecular docking; Nitro-substitution; Potassium-channel. The article conveys some information:
A series of six 3-aryl-6-(N-methylpiperazin)-1,2,4-triazolo[3,4-a]phthalazines were prepared through a facile and efficient one-pot copper-catalyzed procedure from 4-chloro-1-phthalazinyl-arylhydrazones with relatively good yields (62-83%). The one-pot copper-catalytic procedure consists of two simultaneous reactions: (i) a direct intramol. dehydrogenative cyclization between ylidenic carbon and adjacent pyrazine nitrogen to form 1,2,4-triazolo ring and, (ii) a direct N-amination on carbon-chlorine bond. Then, an in vitro anticancer evaluation was performed for the synthesized compounds against five selected human cancer cells (A549, MCF-7, SKBr3, PC-3 and HeLa). The nitro-derivatives were significantly more active against cancer strains than against the rest of tested compounds Specifically, compound I was identified as the most promising anticancer agent with significant biol. responses and low relative toxicities on human dermis fibroblast. The cytotoxic effect of compound I was more significant on PC3, MCF-7 and SKBr3 cancer cells with low-micromolar IC50 value ranging from 0.11 to 0.59μM, superior to Adriamycin drug. Mechanistic exptl. and theor. studies demonstrated that compounds I act as a K+ channel inhibitor in cancer models. Further mol. docking studies suggest that the EGFR Tyrosine Kinase enzyme may be a potential target for the most active 3-aryl-6-(N-methylpiperazin)-1,2,4-triazolo[3,4-a]phthalazines. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 1-Methylpiperazine)
1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 1-Methylpiperazine
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics