Dynamic Anticounterfeiting Through Novel Photochromic Spiropyran-Based Switch@Ln-MOF Composites.

Fluorescent materials presenting unique color changes in response to external stimuli have wide applications in information storage and anticounterfeiting. However, developing intelligent fluorescent materials with high security levels and dynamically displaying encrypted information is still a challenge. Herein, we report a new method for constructing excellent fluorescent materials by loading the photochromic molecule spiropyran into a lanthanide metal-organic framework. Controlling the isomerization of the spiropyran unit regulates the fluorescence resonance energy transfer (FRET) mechanism between the spiropyran acceptor and the lanthanide donor, leading to an exceptional reversible absorption/luminescence modulation ability. As the irradiation time is extended, the fluorescent color changes continuously from yellow-greenish to orange and then to red through the FRET process within 60 s. This composite system has great potential in anticounterfeiting because of the following advantages: (1) the materials have different fluorescence emissions and optical colors regulated by ultraviolet radiation, which is convenient for designing complex anticounterfeiting patterns; (2) the system can be repeatedly verified quickly and exhibit dynamic fluorescence color within 60 s, having great potential in advanced anticounterfeiting, where time is key in encryption/decryption. These unique advantages will greatly enhance the reliability of anticounterfeiting measures and increase the difficulty of anticounterfeiting.

Discovery of N-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2.

Androgen receptor (AR) antagonists have been widely used for the treatment of prostate cancer (PCa). As a link between the AR and its transcriptional function, the activation function 2 (AF2) region has recently been revealed as a novel targeting site for developing AR antagonists. Here, we reported a series of N-(4-(benzyloxy)-phenyl)-sulfonamide derivatives as new-scaffold AR antagonists targeting the AR AF2. Therein, compound T1-12 showed excellent AR antagonistic activity (IC50 = 0.47 µM) and peptide displacement activity (IC50 = 18.05 µM). Furthermore, the in vivo LNCaP xenograft study confirmed that T1-12 offered effective inhibition on tumor growth when administered intratumorally. The study represents the first successful attempt to identify a small molecule targeting the AR AF2 with submicromolar AR antagonistic activity by structure-based virtual screening and provides important clues for the development of novel therapeutics for PCa treatment.

Achieving enhanced solid-state photochromism and mechanochromism by introducing a rigid steric hindrance group.

For photochromic molecules, effective isomerization usually requires conformational freedom, which is usually unavailable under solvent-free conditions. In this work, we report a new method, which can realize the reversible switching of spiropyran molecules by introducing a rigid aromatic ring group and this method can provide the required free volume to transform from a closed-ring to an open-ring form. This new molecule can quickly change color in the solid state under ultraviolet light, and can be erased after being heated at 60 °C for about 5 minutes. Furthermore, this new compound presents mechanochromicity when a mechanical force is applied. What is more, it can be used for at least 30 cycles of print-erase operations without apparent fatigue. This new molecule exhibits improved photochromic and anti-fatigue properties in the solid state, which can promote its application in both ultraviolet printing and anti-counterfeiting materials.