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Transformative reactions in nitroarene chemistry: C-N bond cleavage, skeletal editing, and N-O bond utilization.
Org Biomol Chem
January 2025
Department of Applied Chemistry, Waseda University, 513 Wasedatsurumakicho, Shinjuku, Tokyo 162-0041, Japan.
Nitroarenes are highly versatile building blocks in organic synthesis, playing a pivotal role in various reactions. Common transformations involving nitroarenes include nucleophilic aromatic substitution (SAr) reactions, where the nitro group functions both as a potent electron-withdrawing group that activates the aromatic ring and as a leaving group facilitating the substitution. Additionally, the direct transformation of nitro groups, such as reduction-driven syntheses of amines and carboxylic acids, as well as -substitution SAr reactions, have been extensively explored.
View Article and Find Full Text PDFRemodeling tumor microenvironment by versatile nanoplatform orchestrated mechanotherapy with chemoimmunotherapy to synergistically enhance anticancer efficiency.
Biomaterials
January 2025
School of Pharmacy, Shandong Second Medical University, Weifang, 261053, China. Electronic address:
Solid tumors (particularly the desmoplastic ones) usually harbor insurmountable mechanical barriers and formidable immunosuppressive tumor microenvironment (TME), which severely restricted nanomedicine-penetration and vastly crippled outcomes of numerous therapies. To overcome these barriers, a versatile nanoplatform orchestrated mechanotherapy with chemoimmunotherapy was developed here to simultaneously modulate tumor physical barriers and remodel TME for synergistically enhancing anticancer efficiency. Dexamethasone (DMS) and cis-aconityl-doxorubicin (CAD) were co-hitchhiked into phenylboronic acid functionalized polyethylenimine (PEI-PBA) carrier, and further in situ shielded by aldehyde-modified polyethylene glycol (PEG) to form CAD/DMS@PEG/PEI-PBA (CD@PB) nanoparticles (NPs).
View Article and Find Full Text PDFThio-ProTide strategy: A novel HS donor-drug conjugate (DDC) alleviates hepatic injury innate lysosomal targeting.
Acta Pharm Sin B
December 2024
Key Laboratory of Drug Metabolism and Pharmacokinetics, Research Unit of PK-PD Based Bioactive Components and Pharmacodynamic Target Discovery of Natural Medicine of Chinese Academy of Medical Sciences, China Pharmaceutical University, Nanjing 210009, China.
Hydrogen sulfide (HS) is a gas signaling molecule with versatile bioactivities; however, its exploitation for disease treatment appears challenging. This study describes the design and characterization of a novel type of HS donor-drug conjugate (DDC) based on the thio-ProTide scaffold, an evolution of the ProTide strategy successfully used in drug discovery. The new HS DDCs achieved hepatic co-delivery of HS and an anti-fibrotic drug candidate named hydronidone, which synergistically attenuated liver injury and resulted in more sufficient intracellular drug exposure.
View Article and Find Full Text PDFTumor-Resident Intracellular Bacteria Scavenger Activated In Situ Vaccines for Potent Cancer Photoimmunotherapy.
Adv Healthc Mater
January 2025
Department of Pharmaceutics, School of Pharmacy, Qingdao University, Qingdao, 266071, China.
In situ tumor vaccines, which utilize antigens generated during tumor treatment to stimulate a cancer patient's immune system, has become a potential field in cancer immunotherapy. However, due to the immunosuppressive tumor microenvironment (ITME), the generation of tumor antigens is always mild and not sufficient. Tumor-resident intracellular bacteria have been identified as a complete tumor microenvironment component to contribute to creating ITME.
View Article and Find Full Text PDFCoacervate vesicles assembled by liquid-liquid phase separation improve delivery of biopharmaceuticals.
Nat Chem
January 2025
State Key Laboratory of Advanced Drug Delivery and Release Systems, Liangzhu Laboratory, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
Vesicles play critical roles in cellular materials storage and signal transportation, even in the formation of organelles and cells. Natural vesicles are composed of a lipid layer that forms a membrane for the enclosure of substances inside. Here we report a coacervate vesicle formed by the liquid-liquid phase separation of cholesterol-modified DNA and histones.
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