4364-06-1Relevant articles and documents
Acid-responsive nanoparticles as a novel oxidative stress-inducing anticancer therapeutic agent for colon cancer
Zhao, Chengwei,Cao, Weilan,Zheng, Hailun,Xiao, Zhongxiang,Hhu, Jie,Yang, Lehe,Chen, Min,Liang, Guang,Zheng, Suqing,Zhao, chengguang
, p. 1597 - 1618 (2019)
Objective: Nanoparticles can efficiently carry and deliver anticancer agents to tumor sites. Mounting evidence indicates that many types of cancer cells, including colon cancer, have a weakly acidic microenvironment and increased levels of reactive oxygen species. The construction of nano drug delivery vehicles “activatable” in response to the tumor microenvironment is a new antitumor therapeutic strategy. Methods: Cinnamaldehyde (CA) was designed to link directly with dextran to form a polymer through an acid cleavable acetal bond. Herein, a novel pH-sensitive drug delivery system was constructed with co-encapsulated 10-hydroxy camptothecin (HCPT). Dynamic light scattering (DLS) analysis, transmission electron microscopy (TEM) analysis, and release kinetics analysis of HCPT-CA-loaded nanoparticles (PCH) were conducted to investigate the physical and chemical properties. The cellular uptake signatures of the nanoparticles were observed by confocal microscopy and flow cytometry. Cell viability, cell scratch assay, apoptosis assay, and colony formation assay were performed to examine the potent antiproliferative and apoptotic effects of the PCH. The antitumor mechanism of the treatment with PCH was evaluated by Western blotting, flow cytometry, and TEM analysis. The pharmacokinetics of PCH were examined in healthy Sprague Dawley rats within 6 hours after sublingual vein injection. We lastly examined the biodistribution and the in vivo anticancer activity of PCH using the xenograft mouse models of HCT116 cells. Results: Both HCPT and CA were quickly released by PCH in an acidic microenvironment. PCH not only induced cancer cell death through the generation of intracellular reactive oxygen species in vitro but also facilitated the drug uptake, effectively prolonged drug circulation, and increased accumulation of drug in tumor sites. More attractively, PCH exhibited excellent therapeutic performance and better in vivo systemic safety. Conclusion: Overall, PCH not only utilized the tumor microenvironment to control drug release, improve drug pharmacokinetics, and passively target the drug to the tumor tissue, but also exerted a synergistic anticancer effect. The acid-responsive PCH has enormous potential as a novel anticancer therapeutic strategy.
Intermediate substance with acid degradation function, preparation method of same, and polymerizable monomer prepared from intermediate substance
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Paragraph 0054-0058; 0068, (2021/11/27)
The invention discloses an intermediate substance with an acid degradation function and a preparation method of same; whereinthe preparation method of the intermediate substance comprises the following steps: dissolving 2-nitrobenzaldehyde in a proper amount of dichloromethane, if the reaction substance is cinnamyl aldehyde, mixing the substance with trimethyl orthoformate without the help of a dichloromethane solvent with hafnium trifluoromethanesulfonate as a catalyst; then under the condition of room temperature, performing magnetic stirring to obtain the target substance in a very short time. According to the invention, the defects of time consumption, energy consumption, solvent consumption and the like caused by adopting p-toluenesulfonic acid as a catalyst for preparing the substance traditionally are avoided, and the prepared substance has an acid degradation function. Corresponding 2-nitrobenzaldehyde or cinnamyl aldehyde can be obtained through acid degradation, and in addition, the intermediate substance provides convenience for subsequent preparation of polymerizable monomers with an acid degradation function.
1-phosphanorbornene chiral phosphorus catalyst and synthesis method and application thereof
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Paragraph 0030-0032, (2021/05/29)
The invention discloses a 1-phosphanorbornene chiral phosphorus catalyst and a synthesis method and application thereof. The structure of the catalyst is shown in formulas III and III' in the specification. In the formulas, Ar is phenyl, substituted phenyl, naphthyl or substituted naphthyl; preferably, Ar is phenyl, monosubstituted phenyl or naphthyl; more preferably, Ar is phenyl, 4-monosubstituted phenyl or 2-naphthyl; and furthermore, more preferably, Ar is phenyl, 4-methyl phenyl, 4-methoxy phenyl, 4-benzyl phenyl, 4-tert-butyl phenyl, 4-tert-butoxy phenyl phenyl or 2-naphthyl. The catalyst provided by the invention is used as a chiral phosphine catalyst with a novel structure, three completely bound P-C bonds are formed through introduction of a rigid skeleton, the scientific problem that a phosphorus chiral center is easy to racemize is successfully solved, and the phosphorus chiral catalyst can be widely applied to asymmetric reactions such as asymmetric cyclization catalyzed by chiral phosphine, and has a wide commercial application prospect.
Nickel-Catalyzed Chemoselective Acetalization of Aldehydes With Alcohols under Neutral Conditions
Subaramanian, Murugan,Landge, Vinod G.,Mondal, Akash,Gupta, Virendrakumar,Balaraman, Ekambaram
supporting information, p. 4557 - 4562 (2019/08/30)
A molecularly defined NiII-complex catalyzing the chemoselective acetalization of aldehydes with alcohols under neutral conditions is reported. The reaction is general, efficient and showed a wide substrate scope (including aliphatic aldehydes) as well as excellent functional group tolerance. Reusability of the present nickel catalyst is also demonstrated.
