Current Organic Chemistry - Volume 22, Issue 23, 2018

Halides, as important starting materials, construct complex structures and notable structural motifs in natural products and manufactured drugs. Transition-metalcatalyzed halides formation has emerged as a particular approach to generating organohalides, which is predictable to compete as an alternative to more established synthetic methods. This review attempts to provide different methods to catalyze the synthesis of organohalides by using different transition metals, as well as their application in synthetic chemistry.

Cancer is one of the leading causes of death worldwide. Mutation of the cell regulates genes and protein causing cancer. Surgery, radiotherapy, and the use of anticancer agents are the current therapy of cancer despite their side effects. The general area of research relates to heterocyclic chemistry. The purpose of the article is to review the most recent advances in nitrogen-containing heterocyclics as possible chemotherapy agents for cancer. More than 90% of the novel drugs bear heterocyclics and among them, nitrogencontaining heterocyclic compounds show superior pharmaceutical effect than non-nitrogen compounds. Nitrogen-containing compounds, the heart of drug discovery, present a significant and valuable group of molecules that play a chief and vital role in the metabolism of living cells.

The benzimidazole moiety is a privileged heterocyclic nucleus which has been used broadly in medicinal chemistry. Benzimidazole derivatives are useful building blocks for the development of important compounds of biological and therapeutic interest. The developments of facile synthetic routes to achieve access to these molecules are of prime interest, therefore synthetic organic chemists focused to invent an efficient method for the synthesis of benzimidazole derivatives. In recent years, several reports have been evident forthe synthesis of these heterocyclic compounds in the presence of various conditions; like solvent free, reactant immobilized on solid support, microwave irradiation condition, using various solvents and using different catalysts. Therefore in the present review, we tried to represent a systematic survey on various synthetic strategies leading to the synthesis of compounds bearing benzimidazole moiety by the direct condensation reaction carried out between o-phenylenediamine and aromatic aldehydes using differentcatalytic reagents during last 10 years. This review is a brief account of some frequently used methods to synthesize benzimidazole derivatives using different type of catalysts in various conditions.

A series of triazolo-pyridazinone derivatives were prepared through the standard click reactions of 4,6-diphenyl-2-(prop-2-yn-1-yl)pyridazin-3(2H)-one 1, possessing a free terminal alkyne group with a selection of substituted aryl azides 2-9. The cytotoxicity and in vitro anticancer investigation of the new compounds were conducted against four different human tumor cell lines, including breast adenocarcinoma MCF-7, hepatocellular carcinoma HepG2, lung cancer A549 and colon cancer HCT116 cell lines. The results showed that the compounds exerted their actions in MCF-7 and A549 via inhibition of the urokinase activity. The compound 17 showed potent anticancer activity compared with the activity of the standard anticancer drug, doxorubicin. Molecular docking studies were performed to support the activity data and predict the plausible mechanisms of the ligand-protein interactions.

A series of resorcinarene-PAMAM-porphyrin dendrimers was synthesized. The nanostructures were characterized by IR, 1H and 13C NMR, UV-vis absorption, electrospray ionization and MALDI-TOF mass spectrometry. The morphological properties were characterized by High-Resolution Transmission Electron Microscopy (HRTEM). The distance between the resorcinarene group and the porphyrin group was variable: two different lengths of the dendritic branches were synthesized, which were found to play an important role in influencing the fluorescence properties. It was also possible to observe by HRTEM microscopy that the dendrimers were nearly monodisperse, retained their size and their shape was roughly spherical. Experimental data confirmed that the PAMAM groups favored the intense emission and red shift of the maximum wavelength. It is possible that the fluorescence centers were perturbed by the inner influence between the PAMAM groups. These nanostructures could be used for the conversion of photoenergy.