73043-80-8Relevant articles and documents
A fast-acting reagent for accurate analysis of RNA secondary and tertiary structure by SHAPE chemistry
Mortimer, Stefanie A.,Weeks, Kevin M.
, p. 4144 - 4145 (2007)
Selective 2′-hydroxyl acylation analyzed by primer extension (SHAPE) chemistry allows local nucleotide flexibility to be quantitatively assessed at single nucleotide resolution in any RNA. SHAPE chemistry exploits structure-based gating of the nucleophili
Doxorubicin-loaded polymeric micelle as well as preparation method and application thereof
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, (2020/10/04)
The present invention discloses a doxorubicin-loaded polymeric micelle as well as a preparation method and application thereof. Novel amino evodiamine is adopted to react with polyethylene glycol, a micelle obtained by self-assembly is used as a carrier to load doxorubicin, a prepared mPEG-CO-NH-EVO micelle and a mPEG-CO-NH-EVO-OCH3 micelle have low toxicity to normal hepatocytes so that the two amphipathic polymeric micelles are used as carriers to load DOX to prepare DOX-loaded polymeric micelles, namely a mPEG-CO-NH-EVO/DOX micelle and a mPEG-CO-NH-EVO-OCH3/DOX micelle, and DOX enters hydrophobic shells of the micelles due to the dialysis effect; shapes of the micelles are represented by using a transmission electron microscope and a scanning electron microscope, and the drug loading efficiency and encapsulation efficiency of DOX are tested and calculated by using an ultraviolet spectrophotometer; and finally, evaluating the cytotoxicity by using a CCK-8 method. Shown by cytotoxicity tests, a DOX-loaded polymer has an effect on inhibiting breast cancer cells and particularly has greatly reduced toxicity to the normal hepatocytes.
Synthesis and antimicrobial activity of novel 4-Hydroxy-2-quinolone analogs
Khamkhenshorngphanuch, Thitiphong,Kulkraisri, Kittipat,Janjamratsaeng, Alongkorn,Plabutong, Napasawan,Thammahong, Arsa,Manadee, Kanitta,Na Pombejra, Sarisa,Khotavivattana, Tanatorn
, (2020/07/30)
Alkyl quinolone has been proven to be a privileged scaffold in the antimicrobial drug discovery pipeline. In this study, a series of new 4-hydroxy-2-quinolinone analogs containing a long alkyl side chain at C-3 and a broad range of substituents on the C-6 and C-7 positions were synthesized. The antibacterial and antifungal activities of these analogs against Staphylococcus aureus, Escherichia coli, and Aspergillus flavus were investigated. The structure-activity relationship study revealed that the length of the alkyl chain, as well as the type of substituent, has a dramatic impact on the antimicrobial activities. Particularly, the brominated analogs 3j with a nonyl side chain exhibited exceptional antifungal activities against A. flavus (half maximal inhibitory concentration (IC50) = 1.05 μg/mL), which surpassed that of the amphotericin B used as a positive control. The antibacterial activity against S. aureus, although not as potent, showed a similar trend to the antifungal activity. The data suggest that the 4-hydroxy-2-quinolone is a promising framework for the further development of new antimicrobial agents, especially for antifungal treatment.