5-(4-Hydroxy-1,3-dioxoisoindolin-2-yl)-2,3-dihydrophthalazine-1,4-dione (HDDD) as effective substrate in HRP-catalyzed enhanced chemiluminescence reaction.

By modifying the amino group of luminol, 5-(4-hydroxy-1,3-dioxoisoindolin-2-yl)-2,3-dihydrophthalazine-1,4-dione (HDDD) was synthesized. Using a combination of full factorial design and "one-variable-time" method, favorable conditions for the generation of HDDD-dependent chemiluminescence were determined. It was shown that replacing luminol with HDDD in the HRP-C-catalyzed enhanced chemiluminescence reaction increased the luminescence intensity.

3,4-Diarylisoxazoles-Analogues of Combretastatin A-4: Design, Synthesis, and Biological Evaluation and .

Focusing on the molecular docking results, a series of 3,4-diarylisoxazoles, analogues of Combretastatin A4, bearing various substituents at the fifth position of the isoxazole ring and pharmacophore groups bioisosteric to methoxy substituent at ring B, were synthesized in good yields and high regioselectivity. Depending on the substituent at C5, three approaches were chosen for the construction of isoxazole ring, including nitrosation of gem-dihalocyclopropanes, nitrile oxide synthesis, and difluoromethoxylation of isoxazolone to afford 5-haloisoxazoles, 5-unsubstituted isoxazoles, and 5-difluoromethoxyisoxazoles, respectively. Isoxazoles and showed selective cytotoxicity and antitubulin inhibition properties , with pharmacodynamic profiles closely related to that of CA-4.

RNHal/NOHSO: A Usable System for Halogenation of Isoxazoles, Pyrazoles, and Beyond.

A new convenient and versatile halogenating system (RNHal/NOHSO), giving straightforward and general access to halogenated 3,5-diaryl- and alkylarylisoxazoles, pyrazoles and electron-rich benzenes from the corresponding scaffolds, is suggested. The method provides excellent regioselectivity, scalability to the gram scale, and a broad scope for both aromatics and halogens. A three-step, one-pot reaction protocol was developed, and a series of 3,5-diaryl-4-haloisoxazoles has been efficiently synthesized from 1,2-diarylcyclopropanes under suggested nitrosating-halogenating conditions.