Latest ArticlesExtensive structure-activity relationships (SARs) study of JND3229 was conducted to yield a series of new reversible 2-oxo-3, 4-dihydropyrimido[4, 5-d]pyrimidine privileged scaffold as EGFRC797S inhibitors. One of the most potent compound 6i potently suppressed EGFRL858R/T790M/C797S kinase with an IC50 value of 3.1 nmol/L, and inhibited the proliferation of BaF3 cells harboring EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S mutants with IC50 values of 290 nmol/L and 316 nmol/L, respectively. Further, 6i dose-dependently induced suppression of the phosphorylation of EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S in BaF3 cells. Compound 6i may serve as a promising lead compound for further drug discovery overcoming the acquired resistance of non-small cell lung cancer (NSCLC) patients.
We herein propose a co-delivery approach where small interference RNA (siRNA) and anticancer chemotherapeutic drug are simultaneously loaded into a single delivery carrier for the combined treatment of breast cancer and metastasis prevention. The co-delivery vector is composed of chondroitin sulfate (CS)-coated β-cyclodextrin-polyethylenemine polymer, which is capable of loading paclitaxel (PTX) and siRNA simultaneously to form therapeutic nanocomplexes. The nanocomplex, termed as CPPTX-siCD146-CS, is demonstrated to have strong active targeting ability towards CD44-overexpresing breast cancer cells. Moreover, the co-delivery of PTX and siRNA not only effectively inhibits cancer cells proliferation and induces apoptosis, but also well prevents metastasis. Importantly, CP-PTX-siCD146-CS nanocomplexes exhibit stronger cytotoxic effects and anti-metastatic effects on MBA-MD-231 breast cancer cells, in comparison with PTX or siCD146 mono-treatment. The current study defines a potential therapeutic strategy for the combined breast cancer treatment and metastasis prevention from a codelivery perspective.
Insect chitinase and N-acetyl-β-D-hexosaminidases (Hex) are potential targets for developing new pesticides. Here, a series of thiazolylhydrazones I (with substituted group R1 at N3) and II (with substituted group R1 at N2) were designed, synthesised and evaluated as competitive inhibitors of OfHex1 and OfChi-h, from the agricultural pest Ostrinia furnacalis. Derivatives I-3d and II-3d, with phenoxyethyl group at R1, demonstrated the best inhibitory activities against OfHex1 and OfChi-h. Molecular docking analysis indicated that the branched conformation compound II-3d (Ki=1.5 μmol/L) formed more hydrogen bonds with OfHex1 than the stretched conformation compound I-3d (Ki=5.9 μmol/L). The differences in compounds' binding conformations with OfChi-h explained differences in inhibitory activity of compounds I-3d (Ki=1.9 μmol/L) and II-3d (Ki=4.1 μmol/L). This work suggests a novel scaffold for developing specific Hex and Chi-h inhibitors.
In this study, flower-like MoS2 constructed by nanosheets was synthesized by a simple hydrothermal method. The hydrothermal process was optimized and the effects of hydrothermal condition, including reaction temperature, reaction time and the ratio of Mo source to S source (Mo:S) in precursor, on microwave absorption performances and dielectric properties were investigated. Our results showed that when the reaction temperature was 180℃, the reaction time was 18 h, and the Mo:S was 1:3.5, the synthesized MoS2 had the best performance:Its minimum reflection loss could reach -55.78 dB, and the corresponding matching thickness was 2.30 mm with a wide effective bandwidth of 5.17 GHz. Further researches on the microwave absorption mechanism revealed that in addition to the destructive interference of electromagnetic waves, various polarization phenomena such as defect dipole polarization were the main reasons for microwave loss. We believe that MoS2 is a candidate for a practical microwave absorbent.
(+)-6-3'a, 7-6'-Isowallichilide and (-)-6-3'a, 7-6'-isowallichilide, a pair of enantiomeric phthalide dimers featuring new 6-3'a, 7-6' dimerization sites, were isolated from Ligusticum chuanxiong. The structures were elucidated by NMR spectroscopy and X-ray diffraction analysis. Furthermore, the absolute configurations were assigned using experimental and theoretical electronic circular dichroism methods. Their nitric oxide inhibition, antiplatelet aggregation and antioxidant activities were investigated.
Inflammation, as the pathophysiological response of body to harmful stimuli, leads to changes in cellular microenvironment. To research pH changes in lysosomes of macrophages during inflammation, we designed a FRET (Förster resonance energy transfer) based probe, BDP-RhB. The probe showed good lysosome targeting ability, wide response range of pH from 8.0 to 4.0 with significant ratio (I582/I518) change from 0.6 to 3.4, and good reversibility and sustainability. By applying BDP-RhB, we found a decrease of lysosomal pH of macrophages during inflammation.
Herein we wish to propose the concept of "element-transfer reaction", which may afford the access to elemental compounds by transferring certain elements from easily available resources efficiently, concisely and precisely. A good element-transfer reaction with industrial application potential shall not generate waste and is performed under energy-saving and environment-friendly conditions. During the past decade, we have developed a series of methods for the synthesis of fluorine-and seleniumcontaining compounds via the fluorine-and selenium-transfer reactions, while the redox reactions were considered to be the oxygen-and hydrogen-transfer reactions as well and were also widely studied by our group for producing the high-value-added fine chemicals. Some of these technologies have been successfully industrialized. This review summarizes our staged research results on fluorine-, oxygen-, hydrogen-and selenium-transfer reactions and makes a prospect on the developing trend in the field.
In this study, we report a new small molecule acceptor (named TT-4F) which uses 3, 6-dimethoxylthieno[3, 2-b]thiophene (TT) as the π-bridge. Addition of 0.05 weight ratio amount of TT-4F into the host binary blend of PTB7-Th:IEICO-4F, resulting in a ternary blend in a weight ratio of 1:1:0.05, enables increased open-circuit voltage (Voc), short-circuit current-density (Jsc), and fill-factor (FF) at the same time. Finally, 12.1% efficiency is obtained. Compared to the 3-(2-ethylhexyloxylthiophene) bridge on IEICO-4F, the additional methoxyl group on the TT-6 position is involved in the lowest unoccupied molecular orbital (LUMO) and the larger π-system on TT increases the electron-donating nature, both of which help to raise the LUMO level, one reason of the increased Voc. Upon addition of 0.05 TT-4F, the hole mobility is increased, the monomolecular recombination is reduced, and the charge dissociation and collection is enhanced. All of these contribute to the increased Jsc and FF.
Near-infrared (NIR) light-triggered photothermal therapy (PTT) is a promising treatment strategy for treating cancer. The combination of nanotechnology and NIR has been widely applied. However, the therapeutic efficacy of the drug-delivery system depends on their ability to avoid phagocytosis of endothelial system, cross the biological barriers, prolong circulation life, localize and rapidly release the therapeutic at target sites. In this work, we designed a platelet membrane (PM)-camouflaged hollow mesoporous bismuth selenide nanoparticles (BS NPs) loading with indocyanine green (ICG) (PM@BS-ICG NPs) to achieve the above advantages. PM-coating has active tumor-targeting ability which could prevent drug leakage and provide drug long circulation, causing drug delivery systems to accumulate in tumor sites effectively. Moreover, as a type of the photothermal sensitizers, BS NPs are used as the inner cores to improve ICG stability and are served as scaffolds to enhance the hardness of this drug delivery system. For one hand, the thermal vibration of BS NPs under NIR laser irradiation causes tumor inhibition through hyperthermia. For another hand, this hyperthermia process could damage PM and let ICG rapid release from PM@BS-ICG NPs. The in vitro and in vivo results showed that this biomimetic nano-drug delivery system exhibits obvious antitumor activity which has good application prospect.
Partially biobased polysilylethers (PSEs) are synthesized via dehydrocoupling polymerization catalyzed by an anionic iridium complex. Different types (AB type or AA and BB type) of monomers are suitable. Levulinic acid (LA) and succinic acid (SA) have been ranked within the top 10 chemicals derived from biomass. BB type monomers (diols) derived from LA and SA have been applied to the synthesis of PSEs. The polymerization reactions employ an air-stable anionic iridium complex bearing a functional bipyridonate ligand as catalyst. Moderate to high yields of polymers with number-average molecular weights (Mn) up to 4.38× 104 were obtained. A possible catalytic cycle via an Ir-H species is presented. Based on the results of kinetic experiments, apparent activation energy of polymerization in the temperature range of 0-10 ℃ is about 38.6 kJ/mol. The PSEs synthesized from AA and BB type monomers possess good thermal stability (T5=418 ℃ to 437 ℃) and low glass-transition temperature (Tg=-49.6 ℃).
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