30163-82-7Relevant academic research and scientific papers
COMPOSITIONS FOR TRANSFECTING A NUCLEIC ACID MOLECULE INTO A CELL COMPRISING HETEROCYCLIC COMPOUNDS GRAFTED TO A CATIONIC POLYMER, AND THEIR APPLICATIONS
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Page/Page column 43; 44; 49, (2021/02/12)
The present invention relates to compositions for transfecting a nucleic acid molecule into a cell and their applications. The present invention is directed to a composition suitable for transfecting a nucleic acid molecule into a cell, preferably a eukaryotic cell, comprising (i) at least one compound of general formula (II) or a tautomer, mesomer, racemate, enantiomer, diastereomer, or mixture thereof, or an acceptable salt thereof, and (ii) an acceptable excipient, buffering agent, cell culture medium, or transfection medium, wherein Y11, Y22, Y33, Z11, Z22, Z33, Z44, Z55, Z66, Z77, X11, X22, R33, P++, R, T, U and V are as defined in the description. The present invention also relates to uses of said composition and to a method for in vitro or ex vivo transfection of live cells.
Design, synthesis and preliminary bioactivity evaluations of 8-hydroxyquinoline derivatives as matrix metalloproteinase (MMP) inhibitors
Chen, Chen,Yang, Xinying,Fang, Hao,Hou
, (2019/08/13)
Matrix metalloproteinases (MMPs) play important roles in many diseases including cancer. With moderate metal-binding affinity, 8-hydroxyquinoline has gained much interest in current drug design and development. Specially, it has been reported that 8-hydroxyquinoline derivatives serve as MMP-2 inhibitors with micromolar IC50 values. In the current study, a series of 8-hydroxyquinoline derivatives were designed and synthesized as new MMP-2 and MMP-9 inhibitors. The most active compounds 5e and 5h not only displayed good inhibitory activities against MMP-2/9 with IC50 at submicromolar level, but also possessed potent anti-proliferative, anti-invasive and anti-angiogenesis activity in A549 cell line. Western blot also revealed that 5e and 5h down-regulate the expression of MMP-2 and MMP-9 in A549 cell line. Moreover, flow cytometry analysis indicated that compound 5e could promote apoptosis of A549 cells in vitro. Molecular docking analysis also revealed favorable binding modes of 5e in the active sites of MMP-2 and MMP-9.
SYNTHESIS AND APPLICATION OF IMIDAZOLE DERIVATIVES. SYNTHESIS OF PYRIDOBENZIMIDAZOLONE DERIVATIVES
Ohta, Shunsaku,Yuasa, Teruyuki,Narita, Yoshihiro,Kawasaki, Ikuo,Minamii, Eiji,Yamashita, Masayuki
, p. 1923 - 1931 (2007/10/02)
Pyrido>benzimidazole derivatives (12a and 19a) were synthesized in moderate yields via an intramolecular aldol-condensation of 2-acetyl-1-formylbenzimidazole (11) and an intramolecular acylation of the acylimidazolide (18) prepared from 2-ethoxycarbonylmethyl-1-(2-carboxyethyl)benzimidazole (17), respectively.
