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Development and assessment of novel all-in-one parenteral formulations with integrated anticoagulant properties for the concomitant delivery of 5-fluorouracil and calcium folinate
Initial studies on novel all-in-one formulations of 5-fluorouracil and folinic acid incorporating either sulfated or hydroxypropyl &bgr;-cyclodextrins at physiological pH that potentially address issues of phlebitis, catheter blockages, and thromboembolic events are described and compared. Expand
Aryl Nitro Reduction with Iron Powder or Stannous Chloride under Ultrasonic Irradiation
Abstract The selective reduction of aryl nitro compounds in the presence of sensitive functionalities, including halide, carbonyl, nitrile, and ester substituents, under ultrasonic irradiation at 35Expand
Controlled Delivery of Nitric Oxide for Cancer Therapy
The effects of NO in cancer biology, NO releasing moieties which can be used for NO delivery, and current advances in the design of NO releasing biomaterials focusing on their applications for tumor therapy are covered. Expand
Hypoxia Responsive Drug Delivery Systems in Tumor Therapy.
Four main hypoxia responsive delivery systems are discussed: polymeric based drug delivery systems, oxygen delivery systems combined with radiotherapy and chemotherapy, anaerobic bacteria which are used for delivery of genes to express anticancer proteins such as tumor necrosis alpha (TNF-α) and hypoxIA-inducible transcription factors 1 alpha (HIF1α) responsive gene delivery systems. Expand
Bioorthogonal prodrug activation driven by a strain-promoted 1,3-dipolar cycloaddition† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c4sc02574a
Bioorthogonal prodrug activation controlled by the reaction of a trans-cyclooctene with an azide-functionalized prodrug is presented.
Proteases and protease inhibitors in infectious diseases
This review discusses the chemical and biological makeup of some key druggable proteases expressed by the five major classes of disease causing agents, namely bacteria, viruses, fungi, eukaryotes, and prions and assess the mechanism of action and clinical performance of the protease inhibitors against infectious agents. Expand
Multiple binding modes of isothiocyanates that inhibit macrophage migration inhibitory factor.
A variety of binding modes confirms the existence of two subsites for inhibitors and establishes a platform for the development of potent inhibitors of MIF that only need to target one of these subsites. Expand
Synthesis of reaction-ready 6,6'-biindole and 6,6'-biisatin via palladium(II)-catalysed intramolecular C-H functionalisation.
The first synthesis of a 6,6'-biindole and 6,6'-biisatin scaffold is reported with the penultimate step being the formation of the di-heterocyclic ring by Pd(II)-catalysed intramolecular C-HExpand
Poloxamer 407‐chitosan grafted thermoresponsive hydrogels achieve synchronous and sustained release of antigen and adjuvant from single‐shot vaccines
In vivo, a single dose of CP hydrogel vaccine induced strong, long lasting, cellular and humoral responses that could protect against the development of tumors in a murine melanoma model. Expand
Mechanistic Evaluation of Bioorthogonal Decaging with trans-Cyclooctene: The Effect of Fluorine Substituents on Aryl Azide Reactivity and Decaging from the 1,2,3-Triazoline.
The NMR and computational studies demonstrate that fluorine substituents on the aromatic ring lower the transition state energy required for converting the triazoline to the imine or aziridine intermediates via extrusion of diatomic nitrogen, and that in the case of a tetrafluoro substituted aromatic ring, it is theImine hydrolysis and 1,6-self-immolation decaging that is rate-limiting. Expand