Y06014 is a selective BET inhibitor for the treatment of prostate cancer.

Bromodomain and extra-terminal proteins (BETs) are potential targets for the therapeutic treatment of prostate cancer (PC). Herein, we report the design, the synthesis, and a structure-activity relationship study of 6-(3,5-dimethylisoxazol-4-yl)benzo[cd]indol-2(1H)-one derivative as novel selective BET inhibitors. One representative compound, 19 (Y06014), bound to BRD4(1) in the low micromolar range and demonstrated high selectivity for BRD4(1) over other non-BET bromodomain-containing proteins. This molecule also potently inhibited cell growth, colony formation, and mRNA expression of AR-regulated genes in PC cell lines. Y06014 also shows stronger activity than the second-generation antiandrogen enzalutamide. Y06014 may serve as a new small molecule probe for further validation of BET as a molecular target for PC drug development.

Effect of CaCN2 on the preparation of CaAlSiN3 :Eu2+ phosphors.

Highly efficient red-emitting phosphors, CaAlSiN3 :Eu2+ , were successfully prepared by the solid-state method using calcium cyanide (CaCN2 ) as the single calcium source. The influences of crystallization temperature, crystallization time, calcination mode and compounds ratio on the photoluminescent properties were investigated. The CaAlSiN3 :Eu2+ phosphors were obtained with 1 mol% CaCN2 by a two-step calcination procedure at 900°C for 2 h and subsequently at 1600°C for 8 h. The CaAlSiN3 :Eu2+ phosphors showed the strongest luminescent intensity at 660 nm when excited by 468 nm. With an increase in crystallization time, the maximum wavelength of the emission was shifted from 644 nm to 660 nm.

Organocatalytic sulfa-Michael/aldol cascade: constructing functionalized 2,5-dihydrothiophenes bearing a quaternary carbon stereocenter.

A practical sulfa-Michael/aldol cascade reaction of 1,4-dithiane-2,5-diol and α-aryl-ß-nitroacrylates has been developed, which allows efficient access to functionalized 2,5-dihydrothiophenes bearing a quaternary carbon stereocenter in moderate to good yields with high enantioselectivities.

A new water-soluble phosphorus-dipyrromethene and phosphorus-azadipyrromethene dye: PODIPY/aza-PODIPY.

PODIPY and aza-PODIPY have been successfully prepared by the treatment of dipyrromethene and azadipyrromethene with POCl3 in the presence of Et3 N. The new PODIPY and aza-PODIPY dyes are found to have photophysical properties. PODIPY and aza-PODIPY are water-soluble, and aza-PODIPY is suited for labeling living Hep-2 cells for imaging assays in the near-infrared region. Molecular orbital calculations show that the increase in the HOMO-LUMO band gap for the lowest energy absorption bands is observed in the new phosphorus-containing aza-PODIPY, and the HOMO and LUMO energies of aza-PODIPY are found to be higher than those of aza-BODIPY.

The sol-gel process synthesis of GdAl3(BO3)4:Eu3+ nanophosphors.

GdAl3(BO3)4:Eu3+ red phosphors were prepared using citric acid as complex agent by sol-gel technique. The preparation conditions of the precursor synthesis, including crystallization temperature and crystallization time were investigated. Their structure and luminescence properties were characterized by X-ray diffraction (XRD) analysis and fluorescence spectrometry. The results showed that GdAl3(BO3)4:Eu3+ phosphor crystallized at 960 degrees C for 2 h have been synthesized by sol-gel method. The phosphor is distributed into hexagonal system and the lattice parameters are a = 9.2992 nm c = 7.2577 nm. The excitation spectrum of Gd(0.95)Al3(BO3)4:Eu(0.05)3+ samples is complex and the frequency scale is wide. It consists of a number of main excitation transitions namely 8S(7/2) --> 6IJ (270 nm) of Gd3+, and the others 7F0 --> 5L6 (400 nm), 7F0 --> 5D2 (472 nm) and 7F0 --> 5D1 (542 nm) of Eu3+. The main emission peaks are 614 nm and 619 nm, which are the characteristic emission peaks of Eu3+. These emission peaks correspond to the transition from 5D0 to 7F2 of Eu3+. The shape and the wavelength range of the emission spectrum are similar when the sample was excited by different excitation spectrum. Only the relative intensity of the emission peaks is different from each other.

Study on luminescence behavior of BaAl12O19:Tb, Eu.

BaAl12O19:Tb, Eu phosphors were prepared by sol-gel technique. The luminescence properties and the energy transfer between Eu2+ and Tb3+ were investigated. For BaAll2O19:Tb phosphor, the strongest excitation peak and emission peak produced from Tb3+ transition of 5D4-7F5 were at 240 nm and at 550 nm respectively, while the peak shape was narrow and peak intensity was large. The Eu2+ added in the BaAl12O19:Tb induced energy transfer to Tb3+ and different color luminescence from blue (400 nm) to green (570 nm) was obtained by changing the ratio of Tb3+/Eu2+ with excitation at 240 nm.

Preparation of Eu3+-Y3+ coactivating Na+ based red-emitting luminous materials for light-emitting diodes and investigation of its characteristics.

By solid-state reaction and doping, a series of red-emitting phosphors Na(x)Y(0.92-x/3)(MoO(4))(y)(WO(4))(1-y)O(0.5) : zEu(3+) have been synthesized. Through optimization of the process conditions and photoluminescent analysis, one type of red emission is obtained that matches nicely with ultraviolet light-emitting diode (UV-LED) chips.

Instense red phosphors for UV light emitting diode devices.

Ca(x)Sr1-x-1.5y-0.5zMoO4:yEu3+ zNa+ red phosphors were prepared by solid-state reaction using Na+ as charge supply for LEDs (light emitting diodes). The content of charge compensator, Ca2+ concentration, synthesis temperature, reaction time, and Eu3+ concentration were the keys to improving the properties of luminescence and crystal structure of red phosphors. The photoluminescence spectra shows the red phosphors are effectively excited at 616 nm by 311 nm, 395 nm, and 465 nm light. The wavelengths of 395 and 465 nm nicely match the widely applied emission wavelengths of ultraviolet or blue LED chips. Its chromaticity coordinates (CIE) are calculated to be x = 0.65, y = 0.32. Bright red light can be observed by the naked eye from the LED-based Ca0.60Sr0.25MoO4:0.08Eu3+ 0.06Na+.