A simple catalytic protocol for the synthesis of novel spiro[indoline-pyranodioxine] derivatives has been developed using ZnO nanoparticle as an efficient, green, and reusable catalyst. The derivatives are obtained in moderate to excellent yield by one-pot three-component reaction of an isatin, malononitrile/ethylcyanoacetate, and 2,2-dimethyl-1,3-dioxane-4,6-dione in absolute ethanol under con...

A novel chemical platform based on branched piperazine-2,5-dione derivatives (2,5-diketopiperazines) for creating orally available biologically active peptidomimetics has been developed. The platform includes a diketopiperazine scaffold with "built-in" functionally active peptide fragments covalently attached via linkers. The concept was applied to two hemostimulatory drugs, the dipeptide thymo...

Some new sydnonyl-substituted thiazolidine derivatives were synthesized in high yields by the modified Knoevenagel condensation of 3-aryl-4-formylsydnones with thiazolidine-2,4-dione and 2-thioxo-thiazolidine-4-one, respectively. All the synthesized thiazolidine derivatives were screened by paper-disc method to identify their antimicrobial activities against three bacteria viz. Staphylococcus a...

Thiazacridine and imidazacridine derivatives have shown promising results as tumors suppressors in some cancer cell lines. For a better understanding of the mechanism of action of these compounds, binding studies of 5-acridin-9-ylmethylidene-3-amino-2-thioxo-thiazolidin-4-one, 5-acridin-9-ylmethylidene-2-thioxo-thiazolidin-4-one, 5-acridin-9-ylmethylidene-2-thioxo-imidazolidin-4-one and 3-acrid...

Colorectal cancer (CRC) is a disease with high incidence and mortality, constituting the fourth most common cause of death from cancer worldwide. Naphthoquinones are attractive compounds due to their biological and structural properties. In this work, 36 naphthoquinone derivatives were synthesized and their activity evaluated against HT-29 cells. Overall, high to moderate anti-proliferative act...

In this study, a new series of 6-amino-1,3-dimethyluracil derivative with 6-(3-substituted N-benzylidene)-1,3-dimethyl pyrimidine-2,4-dione-6-yl derivatives which were synthesized by using one pot synthesis. The reaction and different aromatic aldehyde in ethanol yielded Schiff bases (1-6). the subsequent step )1-6) 2-mercaptoacetic acid, 2-chloroacetic acid 2-amino acetic acidn Tetrahydrofuran...

A series of N-[(4-arylpiperazin-1-yl)-alkyl]-2-azaspiro[4.5]decane-1,3-dione derivatives were synthesized and evaluated for their anticonvulsant and neurotoxic properties. The main modifications to that series of compounds consisted in the introduction of an aromatic area to the cyclohexane ring as a flexible fragment with conformational freedom (1a-h), or as a rigidified skeleton (2a-h). Excep...

A simple and ecofriendly method was developed for the synthesis of arylmethylene[bis(5,5- dimethyl-3-hydroxy-2-cyclohexene-1-ones)] from the reaction of 5,5-dimethylcyclohexane- 1,3-dione and aromatic aldehydes in an aqueous media without any catalyst via Knoevenagel condensation followed by rapid Michael addition. No cyclization product was down to convert these enolic forms to xanthene deriva...

One-pot four-component synthesis of polyfunctionalized 1,4-dihydropyridine derivatives was developed by a condensation of aldehydes, malononitrile, diethylacetylenedicarboxylate and aniline in the presence of choline chloride/urea as a deep eutectic solvent (DES)at room temperature.Moreover, an efficient method was reported for the synthesis of highly substituted 4H-chromenes through one-...