CuO nanospindles have been developed to efficiently catalyze the direct arylation of heterocycle C-H bonds with moderate to excellent yields. This reaction can be applied to heterocycles such as benzoxazole, benzothiazole, and 1-methylbenzimidazole in the presence of a more environmentally friendly inorganic base like K(2)CO(3) under ligand-free catalytic conditions. In addition, the catalyst can be recycled and reused without any significant decrease in catalytic activity.

The 1,10-phenanthroline-catalyzed tandem reaction of 2-iodoaniline with isothiocyanate in water is described, which provides an environmentally benign, efficient and simple route for the preparation of 2-aminobenzothiazoles. The present tandem process shows broad substrate scope in the absence of transition metals and phase-transfer catalysts.

A series of novel 3-amido-4-indolylmaleimides have been synthesised from succinimide in five steps sequence consisting of bromination, indole addition, azide substitution, reduction and selective acylation. Cytotoxicity was evaluated for the products against cervical cancer Hela cell lines and human hepatocellular cancer SMMC 7721 cell line by standard MTT assay in vitro. Some ofthese compounds showed moderate cytotoxic potencies.

In an attempt to develop potent and selective antitumor agents, a series of novel 3-amino-4-indolylmaleimides were designed and synthesized. The reaction showed high regioselectivity. The structure of compound 7a was determined by an X-ray single crystal diffraction method. The cytotoxicities of the title compounds were evaluated against HeLa, SMMC 7721 and HL 60 cancer cell lines by a standard MTT assay in vitro. The pharmacological results showed that some of the title compounds displayed moderate or high cytotoxic activity against the tested cell lines. Compound 7d was the most promising compound against the tested cancer cell lines. Structure-activity relationships are discussed based on the experimental data obtained. A hydroxyethylamino group at the 3-position in the side chain of indolylmaleimide is associated with an increase in cytotoxicity.

A series of 1,3-dihydro-2H-3-benzazepin-2-ones with a piperazine moiety were designed and synthesized by treating the common intermediate of 1,3-dihydro-7,8-dimethoxy-3-[3-(1-piperazinyl)propyl]-2H-3-benzazepin-2-ones with a variety of N-aryl-2-chloroacetamides and acyl chlorides. Their structures have been characterized by (1)H-NMR, MS, and elemental analysis. The title compounds were evaluated for their bradycardic activity in vitro. Most of the synthesized compounds exhibited some vasorelaxant activity and heart-rate-reducing activity with bradycardic potency.