105919-36-6Relevant articles and documents
Iridium-catalyzed regio- and enantioselective allylation of ketone enolates
Graening, Timm,Hartwig, John F.
, p. 17192 - 17193 (2005)
The regio- and enantioselective α-allylation of unstabilized ketone enolates with unsymmetrical allylic carbonates to form the branched substitution products in the presence of metallacyclic iridium catalysts is reported. The products, branched γ,δ-unsatu
Synthesis and biological evaluation of coumarin derivatives as α-glucosidase inhibitors
Chen, Jie,Chen, Wen-Hua,Deng, Xu-Yang,Jiang, Zheng-Yun,Li, Dong-Li,Liang, Qi-Ming,Ma, Ai-Jun,Wang, Shao-Hua,Wu, Pan-Pan,Xu, Xue-Tao,Zhang, Kun,Zheng, Xi,Zhou, Ren-Ping
, (2020)
In this study, two series of coumarin derivatives 5a～i and 6a～i were synthesized, and their inhibitory activity against α-glucosidase was determined. The results indicated that most of the synthesized derivatives exhibited prominent inhibitory activities
Piperlongumine analogs promote A549 cell apoptosis through enhancing ROS generation
Li, Peng-Xiao,Li, Yan-Mo,Liu, Guo-Yun,Liu, Ren-Min,Mu, Wen-Wen,Sun, Ai-Ling,Sun, Ya-Lei,Yang, Jie
, (2021)
Chemotherapeutic agents, which contain the Michael acceptor, are potent anticancer molecules by promoting intracellular reactive oxygen species (ROS) generation. In this study, we synthesized a panel of PL (piperlongumine) analogs with chlorine attaching at C2 and an electronwithdrawing/electron-donating group attaching to the aromatic ring. The results displayed that the strong electrophilicity group at the C2–C3 double bond of PL analogs plays an important role in the cytotoxicity whereas the electric effect of substituents, which attached to the aromatic ring, partly contributed to the anticancer activity. Moreover, the protein containing sulfydryl or seleno, such as TrxR, could be irreversibly inhibited by the C2–C3 double bond of PL analogs, and boost intracellular ROS generation. Then, the ROS accumulation could disrupt the redox balance, induce lipid peroxidation, lead to the loss of MMP (Mitochondrial Membrane Potential), and ultimately result in cell cycle arrest and A549 cell line death. In conclusion, PL analogs could induce in vitro cancer apoptosis through the inhibition of TrxR and ROS accumulation.
Base-promoted new C-C bond formation: An expedient route for the preparation of thiazolo- and imidazolo-pyridinones via Michael addition
Yildirim, Muhammet,C?elikel, Derya,Evis, Naciye,Knight, David W.,Kariuki, Benson M.
, p. 5674 - 5681 (2015)
Base-catalyzed one-pot cyclocondensation reactions of acryloyl and cinnamoyl chlorides with β-nitroenamine derivatives have been performed under mild conditions and target 7-substituted thiazolo-[3,2-a] or imidazolo-[1,2-a]pyridin-5-one derivatives were prepared successfully in moderate to good yields. The cyclization reactions may proceed via Michael addition followed by iminoketene-amide tautomerization in view of the products formed.
Photoredox Cyclization of N-Arylacrylamides for Synthesis of Dihydroquinolinones
Liu, Zhaosheng,Zhong, Shuai,Ji, Xiaochen,Deng, Guo-Jun,Huang, Huawen
supporting information, p. 349 - 353 (2021/12/27)
Metal- and additive-free photoredox cyclization of N-arylacrylamides is herein reported that provides a concise access to the formation of dihydroquinolinones. In this protocol, sustainable visible light was used as the energy source, and the organic light-emitting molecule 4CzIPN served as the efficient photocatalyst. This reaction system features exclusive 6-endo-trig cyclization selectivity with a generally good yield of a range of functionalized dihydroquinolinones and dihydrobenzoquinolinones. Mechanistical studies reveal the feasibility of both 1,3-H shift and intersystem crossing of the diradical intermediate.
(E)-4-methyl-2-(4-(trifluoromethyl) styryl) oxazole compound as well as preparation method and application thereof
-
, (2021/06/09)
The invention belongs to the technical field of medicines, relates to a compound with anti-tumor activity and a specific chemical structure, and in particular relates to an (E)-4-methyl-2-(4-(trifluoromethyl) styryl) oxazole compound as well as a preparation method and an application thereof. The structural general formula of the compound is shown in the specification, wherein an R1 group is substituted by a 2-position, 3-position or 4-position mono-substituted fluorine atom, methyl, chlorine atom, methoxy group, bromine atom or an unsubstituted group; and the R2 group is substituted by a 2-position, 3-position or 4-position mono-substituted methoxy group, a chlorine atom or an unsubstituted group. Pharmacological studies show that the compound has certain inhibitory activity on human non-small cell lung cancer A549 cells, can be used for preparing anti-tumor drugs, and opens up a new way for deep research and development of tumor drugs in the future. The preparation method provided by the invention is simple and feasible, relatively high in yield and easy for large-scale production.
