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1.
J Recept Signal Transduct Res ; 36(1): 103-9, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-26416217

RESUMEN

The three-dimensional quantitative structure-activity relationships (3D-QSAR) were established for 30 oxindole derivatives as vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitors by using comparative molecular field analysis (CoMFA) and comparative similarity indices analysis comparative molecular similarity indices analysis (CoMSIA) techniques. With the CoMFA model, the cross-validated value (q(2)) was 0.777, the non-cross-validated value (R(2)) was 0.987, and the external cross-validated value ([Formula: see text]) was 0.72. And with the CoMSIA model, the corresponding q(2), R(2) and [Formula: see text] values were 0.710, 0.988 and 0.78, respectively. Docking studies were employed to bind the inhibitors into the active site to determine the probable binding conformation. The binding mode obtained by molecular docking was in good agreement with the 3D-QSAR results. Based on the QSAR models and the docking binding mode, a set of new VEGFR-2 tyrosine kinase inhibitors were designed, which showed excellent predicting inhibiting potencies. The result revealed that both QSAR models have good predictive capability to guide the design and structural modification of homologic compounds. It is also helpful for further research and development of new VEGFR-2 tyrosine kinase inhibitors.


Asunto(s)
Indoles/química , Simulación del Acoplamiento Molecular , Inhibidores de Proteínas Quinasas/farmacología , Relación Estructura-Actividad Cuantitativa , Receptor 2 de Factores de Crecimiento Endotelial Vascular/antagonistas & inhibidores , Sitios de Unión , Dominio Catalítico , Humanos , Oxindoles , Unión Proteica
2.
Rev Sci Instrum ; 93(6): 064703, 2022 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-35778052

RESUMEN

To solve the problem of the large axial size of high-power microwave (HPM) reflectarray antenna and difficulty in vacuum packaging, a dielectric is introduced in the design of the antenna element. On this basis, a dielectric embedded metasurface reflectarray antenna (DEMRA) with high power handling capacity and wide-range beam scanning capability is proposed and fabricated. Compared with traditional HPM antennas, the DEMRA does not need to be sealed and can work directly in open-air conditions. The DEMRA can realize free regulation of the radiation beam within a cone angle of 90° and has a power handling capacity of 1 GW/m2. As verification, a protype working at 10 GHz is fabricated and low-power experiments are carried out. Experimental results are consistent with the simulation, proving that the DEMRA has a bandwidth exceeding 600 MHz. During the scanning process, the aperture efficiency is always higher than 48.98%, and the side lobe level remains below -15 dB. At the same time, the cross-polarization component is less than -15 dB, while the main lobe-axis ratio remains within 4.5 dB, confirming its beam scanning capability.

3.
Rev Sci Instrum ; 93(8): 084703, 2022 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-36050067

RESUMEN

A beam scanning antenna based on an all-metal lens is presented for high-power microwave (HPM) application in this paper. This design includes a feed antenna and two layers of different all-metal lenses, whose prototypes operating at 14.25 GHz have been successfully designed and fabricated with an aperture radius of 300 mm. A full transmission phase range of 360° can be achieved with a transmission efficiency of over 99% by rotating the cross-slot on the lens elements. The results of the low-power tests depict that the designed antenna can realize a beam scanning range of 120° revolving cone angle with the side lobe below -10 dB and the reflection coefficient less than -16 dB. The high-power tests demonstrate that the power handling capacity of the antenna is higher than 350 MW in sulfur hexafluoride (SF6). In addition, both the designed lenses have a bandwidth of more than 100 MHz. All the merits show that our designed all-metal lens antenna has a great potential to be applied in HPM systems.

4.
Rev Sci Instrum ; 91(11): 114704, 2020 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-33261463

RESUMEN

A novel all-metal phase shifter with continuous linear phase adjustment for high-power microwave applications is presented and tested in this paper. The phase adjustment is achieved through the rotation of a phase reverser for a circularly polarized wave, and the output phase accomplishes a phase adjustment range of 360° by rotating the phase reverser for 180°. Due to the symmetrical characteristics, its position after rotating 180° is the same as the initial position, which can achieve continuous phase adjustment and avoid phase mutation. Simulation results indicate that the phase shifter achieves the transmission efficiency greater than 99.90% at a center frequency of 8.4 GHz, and the bandwidth of transmission efficiency greater than 98.00% is up to 50 MHz. Experiments are carried out and the measured results are in good agreement with simulation. To sum up, the power capacity of this phase shifter is estimated to be more than 80 MW under vacuum conditions (<10-3 Pa), and it can be applied to fast continuous high-power beam-steerable antenna arrays or mode conversion systems.

5.
Rev Sci Instrum ; 90(9): 094704, 2019 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-31575239

RESUMEN

A three-layer aperture coupled microstrip antenna array (ACMA) is designed and fabricated for wideband high-power microwave (HPM) application, which has not been reported in the field of HPM. In this paper, the proposed antenna array overcomes the disadvantage of low power capacity of traditional microstrip antenna arrays. Moreover, based on the H-shaped aperture coupled structure, it enhances the relative bandwidth up to more than 50%. Compared with traditional HPM antennas, it has advantages of being low-profile (less than 0.2λ), wideband, lightweight, and easy to manufacture. The proposed antenna array consists of 60 elements; each element has four aperture coupled patch antennas fed by a four-way microstrip line power divider. In order to realize the modular design, the antenna array is divided into 10 identical modules; benefiting from this design, machining and assembling become easier. Additionally, cold tests and high-power tests are carried out, and the experimental results show that the ACMA achieves a relative bandwidth of 51.2% for voltage standing-wave ratio < 2 from 1.52 to 2.57 GHz. Consistent with simulation results, the measured gain is more than 28.8 dB in the whole bandwidth and it reaches a maximum of 32.1 dB. Finally, the high-power tests show that the power capacity of the proposed ACMA is greater than 140 MW, which proves the feasibility of the design in wideband HPM application.

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