A novel multikinase inhibitor SKLB-YTH-60 ameliorates inflammation and fibrosis in bleomycin-induced lung fibrosis mouse models was written by Liu, Hongyao;Wu, Xiuli;Gan, Cailing;Wang, Liqun;Wang, Guan;Yue, Lin;Liu, Zhihao;Wei, Wei;Su, Xingping;Zhang, Qianyu;Tan, Zui;Yao, Yuqin;Ouyang, Liang;Yu, Luoting;Ye, Tinghong. And the article was included in Cell Proliferation in 2021.Synthetic Route of C14H21BO4 This article mentions the following:
Idiopathic pulmonary fibrosis (IPF) is marked by the excessive accumulation of extracellular matrix, which participates in a variety of chronic diseases or injuries and seriously threatens human health. Due to the side effects of clin. drugs, there is still a need to develop novel and less toxic drugs to treat pulmonary fibrosis. SKLB-YTH-60 was developed through computer-aided drug design, de novo synthesis and high-throughput screening. We employed the bleomycin (BLM)-induced lung fibrosis animal models and used TGF-灏?sub>1 to induce the epithelial-mesenchymal transition (EMT) of A549 cells in vitro. Meanwhile, the protein expression of collagen I and the 浼?smooth muscle actin (浼?SMA), E-cadherin, p-FGFR1, p-PLC绾? p-Smad2/3 and p-Erk1/2 was detected by western blot. YTH-60 has obvious anti-proliferative activity on fibroblasts and A549 cells. Moreover, YTH-60 could impair the EMT of A549 cells and suppressed fibrosis by inhibiting FGFR and TGF-灏?Smad-dependent pathways. I.p. administration of preventive YTH-60 could significantly reduce the degree of fibrosis in mice and regulate the imbalance of the immune microenvironment. In addition, we observed that therapeutic YTH-60 treatment attenuated fibrotic changes in mice during the period of fibrosis. Importantly, YTH-60 has shown an acceptable oral bioavailability (F = 17.86%) and appropriate eliminated half-life time (T1/2 = 8.03 h). Taken together, these preclin. evaluations suggested that YTH-60 could be a promising drug candidate for treating IPF. In the experiment, the researchers used many compounds, for example, 2-(3,5-Dimethoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (cas: 365564-07-4Synthetic Route of C14H21BO4).
2-(3,5-Dimethoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (cas: 365564-07-4) belongs to ethers. Relative to alcohols, ethers are generally less dense, are less soluble in water, and have lower boiling points. They are relatively unreactive, and as a result they are useful as solvents for fats, oils, waxes, perfumes, resins, dyes, gums, and hydrocarbons. Vapours of certain ethers are used as insecticides, miticides, and fumigants for soil. Ethyl ether is an excellent solvent for extractions and for a wide variety of chemical reactions. It is also used as a volatile starting fluid for diesel engines and gasoline engines in cold weather. Dimethyl ether is used as a spray propellant and refrigerant. Methyl t-butyl ether (MTBE) is a gasoline additive that boosts the octane number and reduces the amount of nitrogen-oxide pollutants in the exhaust. The ethers of ethylene glycol are used as solvents and plasticizers.Synthetic Route of C14H21BO4
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem