Four water-soluble hydrazone-based three-dimensional (3D) flexible organic frameworks FOF-1~4 have been synthesized from a semi-rigid tetracationic tetraaldehyde and four flexible dihydrazides. 1H NMR spectroscopy indicated the quantitative formation of FOF-1~4 in D2O, while dynamic light scattering experiments revealed that, depending on the concentration, these porous frameworks display hydrodynamic diameters ranging from 50 nm to 120 nm. The porosity of the frameworks is confirmed by ethanol vapor adsorption experiments of the solid samples as well as the high loading capacity for a 2.3 nm-sized porphyrin guest in water. The new water-soluble frameworks exhibit low cytotoxicity and form inherent pores with diameters of 5.3 nm or 6.7 nm, allowing rapid inclusion of proteins such as bovine serum albumin, green and orange fluorescent proteins, and efficient delivery of the proteins into normal and cancer cells. Flow cytometric analysis reveals percentages of the delivered cells up to 99.8%. Supporting Information The Supporting Information is available free of charge on the ACS Publications website. General methods, synthetic procedures, 1H NMR, IR, DLS, structural modelling, dialysis, cytotoxicity, fluorescence, ITC, CD, CLMS and flow cytometric profiles or images (PDF).
Iridium-complex-incorporated porous organic polymers have been prepared to realize the photocatalysis of four organic transformations with previously unattainable recyclability.
Chemotherapy is one of the main ways to treat breast cancer clinically. However, the multidrug resistance to anti-tumor drugs limits their clinical use. To overcome these drawbacks, the development of drug delivery systems (DDSs) has attracted more and more attention in cancer therapy. At present, the preparation and purification process are complicated for many reported DDSs, while the clinic calls for new DDSs that are more convenient for preparation. Here a new pH-responsive supramolecular organic framework drug delivery complex loading doxorubicin (DOX) is fabricated. Anti-tumor activity of the system in vitro was investigated by cell cytotoxicity, uptake assay, and cell apoptosis analysis. The anti-tumor activity in vivo was investigated by inspecting nude mice body weight, tumor volume and weight, also a preliminary mechanism probe was conducted by HE and TUNEL staining. The DOX@SOF displayed high stability, good biocompatibility and pH-regulated drug release. At acid condition, the hydrazone bonds would be broken, which result in the dissociation of SOF, and then the drugs would be released from the system. Furthermore, DOX@SOF enhanced cellular internalization. Both in vitro and in vivo experiments reflected that DOX@SOF could enhance the anti-tumor activity of DOX. for the MCF-7/ADR tumor cells and tumors. This study provides a highly efficient strategy to prepare a stimulus-responsive supramolecular drug delivery complex for the treatment of drug-resistant cancer, the results presented inspiring scientific interests in exploring new drug delivery strategies and reversing multi-drug resistance for clinical chemotherapy.
Key Points
Question
What is the overall survival benefit of cancer drugs approved in China between 2005 and 2020?
Findings
In this mixed-methods study comprising a systematic review and cross-sectional analysis of 78 cancer drugs for 141 indications, 68 new cancer drug indications approved by Chinese authorities between 2005 and 2020 had documented evidence of overall survival benefit, and 34 did not prolong life.
Meaning
Given regulatory reforms in recent years, these findings highlight the need to routinely monitor the clinical benefits of new cancer therapies in China.
An efficient and facile process was developed for the remote C-H bond amidation of 8-aminoquinoline scaffolds on the C5 position which is geometric. The method only made use of PhI(OAc)2 as a mediator and showed good tolerance toward numerous dibenzenesulfonimides and amides, giving the corresponding products in moderate to excellent yield.
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