Synthesis and evaluation of new chalcones and oximes as anticancer agents was written by Bukhari, Syed Nasir Abbas. And the article was included in RSC Advances in 2022.Category: pyrazines This article mentions the following:
Complex illnesses, such as cancer, are often caused by many disorders, gene mutations, or pathways. Biol. pathways play a significant part in the development of these diseases. Multi-target directed ligands (MTDLs) have been used by medicinal chemists recently in an effort to find single mols. that can affect many targets concurrently. In this work, several chalcones containing the ligustrazine moiety were synthesized and tested for their in vitro anticancer activity and several cancer markers, including EGFR, BRAFV600E, c-Met, and tubulin polymerization, in order to uncover multitarget bioactive compounds In assays using multiple cancer cell lines, the majority of the compounds examined showed strong anticancer activity against them. To synthesize oximes, all of the chalcones were used as precursors. The IC50 values of two compounds ((1Z,2E)-1-(4-(5-Bromothiophen-2-yl)phenyl)-3-(3,5,6-trimethylpyrazin-2-yl)prop-2-en-1-one oxime and (1Z,2E)-1-(4-(4-Methylthiophen-2-yl)phenyl)-3-(3,5,6-trimethylpyrazin-2-yl)prop-2-en-1-one oxime) were found to be 0.87, 0.28, 2.43, 1.04 μM and (1Z,2E)-1-(4-(Thiophen-2-yl)phenyl)-3-(3,5,6-trimethylpyrazin-2-yl)prop-2-en-1-one oxime, 1.47, 0.79, 3.8, 1.63 μM resp., against A-375, MCF-7, HT-29 and H-460 cell lines. These IC50 values revealed an excellent antiproliferative activity compared to those of the pos. control foretinib, (IC50 = 1.9, 1.15, 3.97, and 2.86 μM). Careful examination of their structure and configuration revealed that both compounds had an oxime functional group with z configuration, in place of carbonyl functional group, along with a 2-Ph thiophenyl moiety with or without a bromo group at position-5. The possible binding pattern was implied by docking simulation, inferring the possibility of introducing interactions with the nearby tubulin chain. Since the novel structural trial has been conducted with a detailed structure activity relationship discussion, this work might stimulate new ideas in further modification of multitarget anti-cancer agents and therapeutic approaches. In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3Category: pyrazines).
(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazines are volatile compounds that are used in the cosmetic, food, flavor, and fragrance industries. A large number of pyrazine derivatives are known for their antitumor, antibiotic, anticonvulsant, antituberculosis, and diuretic activities.Category: pyrazines