Mohamed A. Abozeid

Synthesis and antitumor studies of novel benzopyrano-1,2,3-selenadiazole and spiro[benzopyrano]-1,3,4-thiadiazoline derivatives

A convenient and efficient synthetic protocol of new selenadiazole and thiadiazoline derivatives incorporating benzopyranone moiety from readily available starting materials was described. Reaction of different 2,2-dialkyl and 2,2-spirocycloalkyl dihydrobenzopyranones 1a–e with semicarbazide hydrochloride and thiosemicarbazide afforded the corresponding semicarbazones 2a–e and thiosemicarbazones 3a–e, respectively. Furthermore, cyclization of the semicarbazones 2a–e via oxidation using selenium dioxide gave a novel series of chromenoselenadiazoles 4a–e. A series of spirobenzopyrano-1,3,4-thiadidazolines 5a–e were synthesized by refluxing of the thiosemicarbazones 3a–e in acetic anhydride. The synthesized compounds were tested in vitro against four cancer cell lines namely: MCF-7, VERO, WI-38, and HEPG-2. In vivo studies were also performed using Ehrlich ascites carcinoma for antitumor activity. Interestingly, Compounds 4b and 5a showed significant antitumor activities and were capable to improve the hematological parameters as well as increase the mean survival time of the mice bearing tumor.

Developments in 1,2,5-triazepine chemistry: Reactions and synthetic applications

ABSTRACT The chemistry of 1,2,5-triazepines and related compounds is reported. The investigated heterocycles are monocyclic and fused 1,2,5-triazepines. The different sections cover the synthesis and reactions of monocyclic and fused heterocycles incorporating 1,2,5-triazepine ring systems. This review also covers modifications of the 1,2,5-triazepines into many useful ring systems using a host of reagents and other multistep transformations. The biological evaluation of the target compounds is described, as well as the synthetic applications. The reaction mechanisms are discussed. GRAPHICAL ABSTRACT

Enantio- and Diastereoselective Betti/aza-Michael Sequence: Single Operated Preparation of Chiral 1,3-Disubstituted Isoindolines

The first enantio- and diastereoselective Betti/intramolecular aza-Michael sequence carried out using a C3-symmetric chiral trisimidazoline organocatalyst is reported. The reaction of phenols and N-tosylimines bearing a Michael acceptor moiety afforded densely functionalized 1,3-disubstituted isoindolines bearing two stereogenic centers as single diastereomers in high yields (≤93%) and excellent enantioselectivities (≤99.9%).

Advances in 1,3,5-triazepines chemistry

This review describes a literature survey of 1,3,5-triazepines. The investigated heterocycles were the monocyclic and fused 1,3,5-triazepines. The different sections of the paper cover: theoretical methods, spectroscopy aspects, thermodynamic aspects, synthesis and reactions of the monocyclic and fused heterocycles incorporated into the 1,3,5-triazepine moiety. The biological evaluation of the target compounds are also described as well as their synthetic applications. The reaction mechanisms are discussed.

Synthesis, biological evaluation and in silico molecular docking of novel 1-hydroxy-naphthyl substituted heterocycles

Graphical abstract Novel 1-hydroxy-naphthyl substituted heterocycles were synthesized and tested in vitro as antioxidant and antimicrobial agents. In silico molecular docking were performed in order to understand the binding interactions of the molecules with the receptors.