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1.
Angew Chem Int Ed Engl ; 62(16): e202301262, 2023 Apr 11.
Artigo em Inglês | MEDLINE | ID: mdl-36812298

RESUMO

TFA promoted deprotection of O-Ts activated N-Boc hydroxylamines triggers aminofunctionalization-based polycyclizations of tethered alkenes. The processes involve intramolecular stereospecific aza-Prilezhaev alkene aziridination in advance of stereospecific C-N cleavage by a pendant nucleophile. Using this approach, a wide range of fully intramolecular alkene anti-1,2-difunctionalizations can be achieved, including diaminations, amino-oxygenations and amino-arylations. Trends associated with the regioselectivity of the C-N cleavage step are outlined. The method provides a broad and predictable platform for accessing diverse C(sp3 )-rich polyheterocycles of relevance to medicinal chemistry.

2.
Angew Chem Int Ed Engl ; 62(48): e202312797, 2023 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-37846756

RESUMO

Under acidic reaction conditions (TFA), deprotection of BocNR(OSO2 R) reagents triggers intermolecular aminative cyclizations of alkenes equipped with pendant nucleophiles. The processes are predicated on a sequence of stereospecific intermolecular aza-Prilezhaev aziridination followed by stereospecific SN 2-like opening by the pendant nucleophile. The method offers broad scope with respect to the nucleophile (N-, O- or C-based), alkene and cyclization mode, allowing the installation of two contiguous stereocenters under operationally simple conditions.

3.
Opt Express ; 26(17): 22123-22134, 2018 Aug 20.
Artigo em Inglês | MEDLINE | ID: mdl-30130910

RESUMO

In this work, high mobility indium tin oxide (ITO) thin films with uniform crystallographic orientation are prepared. These films present a wide-range transmittance window and could be used as transparent electrodes at ultraviolet-visible-infrared wavelengths. In particular, the ITO thin film is characterized by low resistivity (5.1 × 10-4 Ωcm) and high infrared transmittance (88.5% at 2.5 µm) due to the improved mobility, achieving higher infrared performance than other transparent conductive materials. A model based on carrier's transport theory and Lorentz-Drude dielectric function is proposed to quantitatively calculate the optical performance of conductive thin films under the influence of plasma effect. The calculation demonstrates that ITO is a suitable electrode material for near/middle infrared optoelectronic applications.

4.
Adv Mater ; 36(15): e2307790, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38088221

RESUMO

Applying solar energy into energy storage battery systems is challenging in achieving green and sustainable development, however, the efficient progress of photo-assisted metal-air batteries is restricted by the rapid recombination of photogenerated electrons and holes upon the photocathode. Herein, a 1D-ordered MoS2 nanotube (MoS2-ONT) with confined mass transfer can be used to extend the lifetime of photogenerated carriers, which is capable of overcoming the challenge of rapid recombination of electron and holes. The tubular confined space cannot only promote the orderly separation and migration of charge carriers but also realize the accumulation of charge and the rapid activation of oxygen molecules. The concave surface of MoS2-ONT can improve the carrier separation ability and prolong the carrier lifetime. Meanwhile, the ordered tubular confined space can effectively realize the rapid transfer of charge, ion, and oxygen. Under light irradiation, a fast oxygen reduction reaction kinetics of 70 mW cm-2 for photo-assisted Zn-air battery is achieved, which is the highest value reported for photo-assisted Zn-air batteries. Significantly, the photo-assisted Li-O2 battery based on MoS2-ONT also shows superior rate capability and other exciting battery performance. This work shows the universality of the confined carrier separation strategy in photo-assisted metal-air batteries.

5.
J Med Chem ; 66(15): 10761-10781, 2023 08 10.
Artigo em Inglês | MEDLINE | ID: mdl-37523716

RESUMO

SMARCA2 is an attractive synthetic lethality target for human cancers with SMARCA4 deficiency. Herein, we report the design, synthesis, and biological evaluation of selective SMARCA2 protein degraders developed using the proteolysis targeting chimera (PROTAC) technology. Our efforts have led to the discovery of a series of potent and selective SMARCA2 degraders, exemplified by SMD-3040. SMD-3040 degrades SMARCA2 protein with a low nanomolar DC50 and Dmax > 90% and demonstrates an excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein. It displays potent cell growth inhibitory activity in a panel of SMARCA4-deficient cancer cell lines and has much weaker activity in SMARCA4 wild-type cancer cell lines. SMD-3040 achieves strong tumor growth inhibition in two SMARCA4-deficient xenograft models at well-tolerated dose schedules. Further optimization of SMD-3040 may lead to the discovery of new therapies for the treatment of human cancers with SMARCA4 deficiency.


Assuntos
Mutações Sintéticas Letais , Fatores de Transcrição , Humanos , Linhagem Celular Tumoral , Proteólise , DNA Helicases , Proteínas Nucleares
6.
Materials (Basel) ; 13(4)2020 Feb 19.
Artigo em Inglês | MEDLINE | ID: mdl-32092875

RESUMO

In this paper, the effect of trace Sn on the precipitation behavior and mechanical properties of Al-Mg-Si alloys with different Mg/Si ratios aged at 180 °C was investigated using hardness measurements, a room-temperature tensile test, transmission electron microscopy and differential scanning calorimetry. The results shown that Sn reduces the precipitation activation energy, increases the number density of ß″ precipitates, and then increased the aging hardenability and mechanical properties of the Al-Mg-Si alloy. However, the positive effect of Sn on the mechanical properties of the Al-Mg-Si alloy drops with the decrease of the Mg/Si ratio of the alloy.

7.
J Trauma Acute Care Surg ; 73(4): 902-7, 2012 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22902731

RESUMO

BACKGROUND: Explosive damages to the maxillofacial bones exhibit complex dynamic response processes; the current traditional model and methods for blast wounds are unable to meet research needs. The finite element (FE) method has obvious advantages in complex biomechanical analysis. The objective of this study was to develop an FE model for blast injuries to the pig mandible and investigate the feasibility of using FE method as an ideal research tool for mandible blast wounds. METHODS: A hexahedral FE model of a pig mandible was established to simulate explosive damage in air by using MIMICS and ANSA software. Then, the FE model was imported into LS-DYNA for computation. Finally, the LS-POST was used for the analysis and the measurements. At the same time, an experimental study was performed by measuring biomechanical data (strains and accelerations) and wound patterns from fresh pig mandibles to validate our FE model and simulation result. RESULTS: The FE model and the dynamic processes of blast injuries to the pig mandible were developed and simulated successfully, and most of the biomechanical data and wound patterns displayed no significant differences with experimental results. Stress distribution in the mandible was relatively uniform; high-intensity strain was mainly concentrated in the mandibular angle and ramus, especially along the location of the fracture line. CONCLUSION: The FE model and method of this experiment will be helpful for investigations in the biomechanical mechanisms of mandibular blast injuries and the subsequent human maxillofacial blast injury simulation.


Assuntos
Traumatismos por Explosões/fisiopatologia , Explosões , Análise de Elementos Finitos , Mandíbula/fisiopatologia , Traumatismos Mandibulares/fisiopatologia , Modelos Biológicos , Estresse Mecânico , Animais , Fenômenos Biomecânicos , Simulação por Computador , Modelos Animais de Doenças , Suínos
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