Theeramunkong, Sewan; Maicheen, Chirattikan; Krongsil, Rinnara; Chaichanasap, Waritsara; Asasutjarit, Rathapon; Vajragupta, Opa published an article in 2022. The article was titled 《Synthesis and in vitro biological evaluation of (iso)quinoline-1,2,3-triazole derivatives as anticancer agents》, and you may find the article in Chemical Papers.Electric Literature of C7H5N The information in the text is summarized as follows:
Two series of triazole derivatives I [Ar = 1-naphthyl, pyridin-3-yl, isoquinolin-4-yl, etc.; R = 2-methoxyphenyl, 4-tert-butylphenyl, 2-cyanophenyl, etc.] were designed and synthesized as potential anticancer agents. A series of eighteen novel 1,2,3-triazole derivatives I were synthesized through copper catalyzed click reaction. The compounds were evaluated for their cytotoxicity activity against HepG2, HeLa cell and HEK293 cell lines using MTT assay. The results showed that compounds [Ar = 4-isoquinolyl; R = 2-methoxyphenyl, 3-cyanophenyl] were the most potent compounds against HepG2 cell with IC50 values 9.6 and 13.3μM, resp. Addnl., the compounds I [Ar = 4-isoquinolyl; R = 2-methoxyphenyl, 3-cyanophenyl] were the most potent compounds against HeLa cell with IC50 values 5.7 and 5.8μM, resp. The results of tubulin polymerization assay demonstrated that lead compound I [Ar = 4-isoquinolyl; R = tert-butyl] and compound I [Ar = 4-isoquinolyl; R = 2-methoxyphenyl] could inhibit in vitro tubulin polymerization In addition, a mechanism study displayed that I [Ar = 4-isoquinolyl; R = 2-methoxyphenyl] blocked cell cycle arrest at G2/M phase. Furthermore, a mol. docking study demonstrated that I [Ar = 4-isoquinolyl; R = 2-methoxyphenyl] could bind to the colchicine site of tubulin and form hydrogen bonds in the active site of β-tubulin. In summary, this study recommended a promising isoquinoline-triazole scaffold for further development as more efficient microtubule polymerization inhibitors in the field of cancer treatment.4-Ethynylpyridine(cas: 2510-22-7Electric Literature of C7H5N) was used in this study.
4-Ethynylpyridine(cas: 2510-22-7) belongs to pyridine. In industry and in the lab, pyridine is used as a reaction solvent, particularly when its basicity is useful, and as a starting material for synthesizing some herbicides, fungicides, and antiseptics.Electric Literature of C7H5N