Synthesis and biological evaluation of novel ligustrazine-chalcone derivatives as potential anti-triple negative breast cancer agents was written by Luo, Yingqi;Wu, Wenhao;Zha, Dailong;Zhou, Wenmin;Wang, Chengxu;Huang, Jianan;Chen, Shaobin;Yu, Lihong;Li, Yuanzhi;Huang, Qinghui;Zhang, Jianye;Zhang, Chao. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2021.Category: pyrazines This article mentions the following:
A series of novel ligustrazine-chalcone hybrids I [R = H, 4-F, 3,5-(MeO)2, etc.] was synthesized and evaluated for their in vitro and in vivo antitumor activities. The results showed that most of these compounds exhibited significant in vitro cytotoxicity against MDA-MB-231, MCF-7, A549 and HepG2 cell lines with IC50 values as low as sub-micromole. Among them, compounds I [R = 4-MeO, 4-F] possessed better comprehensive characteristics for antiproliferation effects on both MDA-MB-231 (IC50: compound I [R = 4-MeO], 1.60 鍗?0.21娓璏; compound I [R = 4-F], 1.67 鍗?1.25娓璏) and MCF-7 (IC50: compound I [R = 4-MeO], 1.41 鍗?0.23娓璏; compound I [R = 4-F], 1.54 鍗?0.30娓璏). They also exhibited potent colony-formation inhibitory abilities on above two cell lines in both concentration and time dependent manners, as well as significantly suppression capabilities against migration of such cell lines in a concentration dependent manner by wound-healing assay. Of note, compound I [R = 4-MeO] could significantly induce apoptosis of MDA-MB-231 cells in a concentration dependent manner and inhibited transformation of growth cycle of MDA-MB-231 cells and blocked cell growth cycle in G0/G1 phase. Moreover, in vivo antiproliferation assay of compound I [R = 4-MeO] on TNBC model indicated such compound had a remarkable potency against tumor growth with a widely safety window. Further immunohistochem. anal. illustrated that compound I [R = 4-MeO] was provided with a potent capacity to significantly reduce Ki-67 pos. rate in a dose dependent manner. All results suggested that these hybrids presented both in vitro and in vivo proliferation inhibition potency against breast cancer and further development with good therapeutic potential should be of great interest. 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. Pyrazine derivatives have antitumor, antibiotic, anticonvulsant, antituberculous and diuretic effects as well as kinase, enzymatic and potent tubulin and FtsZ polymerization inhibitory activities. Pyrazine and a variety of alkylpyrazines are flavor and aroma compounds found in baked and roasted goods. Tetramethylpyrazine (also known as ligustrazine) is reported to scavenge superoxide anion and decrease nitric oxide production in human Granulocytes.Category: pyrazines