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.
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.
One-Pot Preparation of (E)-α,β-Unsaturated Aldehydes by a Julia-Kocienski Reaction of 2,2-Dimethoxyethyl PT Sulfone Followed by Acid Hydrolysis
Ando, Kaori,Watanabe, Haruka,Zhu, Xiaoxian
, p. 6969 - 6973 (2021/05/06)
(E)-α,β-Unsaturated aldehydes were synthesized by the Julia-Kocienski reaction of 2,2-dimethoxyethyl 1-phenyl-1H-tetrazol-5-yl (PT) sulfone 3 with various aldehydes, followed by acid hydrolysis. The reaction could be carried out in one pot, and various (E)-α,β-unsaturated aldehydes were obtained in a short time and with high yields.
Synthesis of (E)-α,β-unsaturated carboxylic esters derivatives from cyanoacetic acid via promiscuous enzyme-promoted cascade esterification/Knoevenagel reaction
Wilk, Monika,Trzepizur, Damian,Koszelewski, Dominik,Brodzka, Anna,Ostaszewski, Ryszard
, (2019/02/25)
A new enzymatic protocol based on lipase-catalyzed cascade toward (E)-α,β-unsaturated carboxylic esters is presented. The proposed methodology consists of elementary organic processes starting from acetals and cyanoacetic acid leading to the formation of desired products in a cascade sequence. The combination of enzyme promiscuous abilities gives a new opportunity to synthesize complex molecules in the one-pot procedure. Results of studies on the influence of an enzyme type, solvent, and temperature on the cascade reaction course are reported. The presented methodology provides meaningful qualities such as significantly simplified process, excellent E-selectivity of obtained products and recycling of a biocatalyst.
