937-62-2Relevant articles and documents
Novel artemisinin derivatives with potent anticancer activities and the anti-colorectal cancer effect by the mitochondria-mediated pathway
Lin, Lan,Lu, Wenyu,Dai, Tianzhi,Chen, Huan,Wang, Tong,Yang, Li,Yang, Xuelian,Liu, Ying,Sun, Dequn
, (2020/12/14)
Many artemisinin derivatives have good inhibitory effects on malignant tumors. In this work, a novel series of artemisinin derivatives containing piperazine and fluorine groups were designed and synthesized and their structures were confirmed by 1H NMR, 13C NMR and HRMS technologies. The in vitro cytotoxicity against various cancer cell lines was evaluated. Among the derivatives, compound 12h was found to exhibit not only the best activity against HCT-116 cells (IC50 = 0.12 ± 0.05 μM), but also low toxicity against normal cell line L02 (IC50 = 12.46 ± 0.10 μM). The mechanisms study revealed that compound 12h caused the cell cycle arrest in G1 phase, induced apoptosis in a concentration-dependent manner, significantly reduced mitochondrial membrane potential, increased intracellular ROS and Ca2+ levels, up-regulated the expression of Bax, cleaved caspase-9, cleaved caspase-3, and down-regulated the expression of Bcl-2 protein. A series of analyses confirmed that 12h can inhibit HCT-116 cells migration and induce apoptosis by a mechanism of the mitochondria-mediated pathway in the HCT-116 cell line. The present work indicates that compound 12h may merit further investigation as a potential therapeutic agent for colorectal cancer.
Versatile Cp*Co(III)(LX) Catalyst System for Selective Intramolecular C-H Amidation Reactions
Chang, Sukbok,Jung, Hoimin,Kim, Dongwook,Lee, Jeonghyo,Lee, Jia,Park, Juhyeon
supporting information, p. 12324 - 12332 (2020/08/06)
Herein, we report the development of a tailored cobalt catalyst system of Cp*Co(III)(LX) toward intramolecular C-H nitrene insertion of azidoformates to afford cyclic carbamates. The cobalt complexes were easy to prepare and bench-stable, thus offering a convenient reaction protocol. The catalytic reactivity was significantly improved by the electronic tuning of the bidentate LX ligands, and the observed regioselectivity was rationalized by the conformational analysis and DFT calculations of the transition states. The superior performance of the newly developed cobalt catalyst system could be broadly applied to both C(sp2)-H and C(sp3)-H carbamation reactions under mild conditions.
Method for industrial production of p-hydroxybenzaldehyde with p-tolyl chloroformate as raw material
-
Paragraph 0013, (2017/12/30)
The invention provides a method for industrial production of p-hydroxybenzaldehyde with p-tolyl chloroformate as a raw material. The method comprises the following steps: reacting phosgene with p-cresol to produce p-tolyl chloroformate; and subjecting a photochemical reaction product to distillation, subjecting p-tolyl chloroformate obtained at tower top to chlorination, and subjecting a substance obtained at tower bottom to alkaline hydrolysis for recovery of p-cresol. According to chlorination of p-tolyl chloroformate, gas chromatography is used for tracing chlorination products; a mixture of monochloride and dichloride is subjected to rectification and separation under high vacuum when the content of dichloride on a methyl group is in a range of 55-70%; the tower-top distillate monochloride and a small amount of dichloride are recycled for chlorination again; tower-bottom dichloride is distilled; then hydrolysis, crystallization, filtering and washing of a crystal with cold desalted water are successively carried out to obtain a p-hydroxybenzaldehyde product with a purity of 99%; after multiple repeated cycles, the yield of the p-hydroxybenzaldehyde product can reach 75%.
