Design, synthesis and antitumor activities of thiazole-containing mitochondrial targeting agents was written by Zhang, Dongdong;Hu, Yixin;Hao, Zhiqiang;Zhang, Yang;Luo, Shuhua;Dang, Xin;Sun, Ran;Duan, Shixin;Lv, Dan;Jiang, Faqin;Fu, Lei. And the article was included in Bioorganic Chemistry in 2021.SDS of cas: 626-64-2 This article mentions the following:
In this study, a novel batch of thiazole-containing mitochondrial targeting agents e.g., I were designed and synthesized. Four kinds of mitochondrial targeting moieties and six kinds of linkers were designed. The screening of antiproliferative activity revealed that most compounds displayed cytotoxicity on HeLa cancer cell. In particular, II has an IC50 value of 35.32μmol·L-1 against HeLa cell. In addition, cellular respiratory activities were also tested on HeLa cancer cells. The II had a basal oxygen consumption rate of 8.84 pmol·s-1·mL-1. Also, II inhibited the mitochondrial respiration of HeLa cell significantly at 5μmol·L-1, as well as a complete inhibitory of oxygen consumption for cellular ATP coupling. Furthermore, the pKa, logP, and logD under different pH conditions of all the compounds were calculated by the ACD/Percepta-PhysChem Suite, and the results manifested the correlation between physicochem. properties and chem. activity of compounds The results identify II as a promising mitochondria inhibitor and anticancer agent with appropriate physicochem. properties. In the experiment, the researchers used many compounds, for example, Pyridin-4-ol (cas: 626-64-2SDS of cas: 626-64-2).
Pyridin-4-ol (cas: 626-64-2) belongs to pyridine derivatives. The ring atoms in the pyridine molecule are sp2-hybridized. The nitrogen is involved in the π-bonding aromatic system using its unhybridized p orbital. The lone pair is in an sp2 orbital, projecting outward from the ring in the same plane as the σ bonds. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. SDS of cas: 626-64-2