Copper-catalyzed 1,3-dipolar cycloaddition of methyleneindolinones and N,N'-cyclic azomethine imines

A copper-catalyzed stereoselective 1,3-dipolar cycloaddition of methyleneindolinones and N,N0-cyclic azomethine imines has been developed under mild reaction conditions.The spiro[pyrazolidin-3,30-oxindoles] were obtained in moderate to high isolated yields（up to 82%） with good stereoselevtivities（up to 15：1） in the presence of 5 mol% of Cu（OAc）2at room temperature.

One-pot synthesis of tetrahydroindoles via a copper catalyzed N-alkynation/[4+2] cycloaddition cascade

A CuSO_4 catalyzed ynamide formation/[4+2] cycloaddition relay reaction was achieved in one-pot.Various 4,7-cis-dihydroindolines were produced in good to high yields. The one-pot operation in conjunction with the cheap and benign copper catalysis renders this reaction highly sustainable.

Ruthenium catalyzed amination cyclization of 1,2,4-butanetriol with primary amines:A borrowing hydrogen strategy for 3-pyrrolidinol synthesis

A ruthenium based catalytic system([Ru(p-cymene)Cl2]2/XantPhos with substoichiometric Cs2CO3)has been established to effectively achieve the first direct amination cyclization of 1,2,4-butanetriol with primary aromatic amines.The product of this sustainable hydrogen autotransfer process is valuable Naryl-3-pyrrolidinol.

A Fluorescent Chemosensor for Al3＋ Based on C=O Isomerization Derivated from Curcumin

A simple and nontoxic fluorescent chemosensor of di-O-methyl curcumin has been prepared from curcumin. The sensor exhibited selective and sensitive fluorescent responses toward A13＋ over a wide range of metal ions, such as Mn2＋, Ce3＋, Pt2＋, Sn4＋, Hg＋, Sb3＋, K＋, Ca2＋, Mg2＋, Ba2＋, Cu2＋＇ Ni2＋＇ Na＋＇ NH4＋＇ Ag＋＇ Pb2＋＇ Zn2＋＇ Fee＋＇ Fe3＋, Hg2＋ and Cr3＋ in ethanol/water. The free ligand showed quite weak fluorescence emission due to the isom- erization of C=O double bond in the excited state, however, after addition of Al3＋, fluorescence emission results in a prominent fluorescence enhancement.

Cell Cycle Arrest, Apoptosis, and Autophagy Induced by chabamide in Human Leukemia Cells

Objective To investigate the antitumor effect of chabamide in K562 （human leukemia cell line） cells. Methods The cytotoxicity was assessed by a standard colorimetric assay using 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyltetrazolium bromide （MTT）. The morphological changes were observed by Hoechst 33258 staining. Induction of apoptosis, loss of the mitochondrial membrane potential （A ~＇m）, and cell cycle analysis were evaluated by flow cytometry （FCM） analysis. Levels of apoptosis-related proteins, ceil cycle-related proteins, and LC3 protein were detected by Western blotting. Moreover, the autophagy induced by chabamide was also detected by MDC fluorescent staining. Results Chabamide significantly inhibited cell proliferation by cell cycle arrest in the Go/G1 phase. This phenomenon was associated with an obvious increase in p21 expression and decrease in cyclin D1 and cyclin-dependent kinase 2/4/6 protein expression. Moreover, chabamide could regulate the changes in mitochondrial membrane potential, increase the expression of apoptosis-related proteins, such as Bax and cytochrome C, and decrease the protein expression of Bcl-2, caspase-9, caspase-3, and PARP-1. JNK, ERK1/2, and p38 were also regulated by chabamide in K562 cells. Furthermore, induction of autophagy, marked by autophagic vacuole formation, was detected. Conversion of LC3-1 to LC3-11, a marker of active autophagosome formation, was also detected following chabamide treatment. Conclusion The antitumor activity of chabamide with the results of apoptosis and autophagy induction was confirmed in K562 cells.