Discovery of potential anticancer multi-targeted ligustrazine based cyclohexanone and oxime analogs overcoming the cancer multidrug resistance was written by Zha, Gao-Feng;Qin, Hua-Li;Youssif, Bahaa G. M.;Amjad, Muhammad Wahab;Raja, Maria Abdul Ghafoor;Abdelazeem, Ahmed H.;Bukhari, Syed Nasir Abbas. And the article was included in European Journal of Medicinal Chemistry in 2017.Formula: C8H12N2O This article mentions the following:
The drug research and development nowadays is focusing on multitarget drugs. In the treatment of cancer, therapies using drugs inhibiting one numerous targets signify a novel viewpoint. In comparison with traditional therapy, multitargeted drugs directly aim cell subpopulations which are involved in progression of tumor. The current study comprises the synthesis of 34 novel ligustrazine-containing α, β-unsaturated carbonyl-based compounds and oximes. The growth of 5 various cancer cell types was strongly inhibited by ligustrazine-containing oximes as revealed by biol. evaluation. A strong SAR was provided by the antiproliferative activity. The mechanistic effects of most active antiproliferative compounds on tubulin polymerization, EGFR TK kinases, KAF and BRAFV600E were investigated, followed by in vitro investigation of reversal of efflux-based resistance developed by cancer cells. EGFR was strongly inhibited by two oximes I and II. Out of all linkers including pos. control, 1-isopropyl-piperidin-4-one linker-bearing compounds showed best inhibition of FAK. The strongest inhibitory activity of BRAFV600E was showed by a compound with an IC50 of 0.7 μM. Several analogs including I exhibited a dual role as anticancer as well as MDR reversal agents. For understanding the target protein integrations with new compounds, mol. docking studies were also carried out. In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3Formula: C8H12N2O).
(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazine is an N-heterocyclic moiety, and it can be easily prepared from ethylenediamine and 1,2-diketone, α-hydroxyketone, α-methyl ketone. A number of pyrazine-based derivatives were used as dyes or fluorescent probes.Formula: C8H12N2O