8-Amino-6-Methoxyquinoline—Tetrazole Hybrids: Impact of Linkers on Antiplasmodial Activity

Abstract

A new series of compounds was prepared from 6-methoxyquinolin-8-amine or its N-(2-aminoethyl) analogue via Ugi-azide reaction. Their linkers between the quinoline and the tert-butyltetrazole moieties differ in chain length, basicity and substitution. Compounds were tested for their antiplasmodial activity against Plasmodium falciparum NF54 as well as their cytotoxicity against L-6-cells. The activity and the cytotoxicity were strongly influenced by the linker and its substitution. The most active compounds showed good activity and promising selectivity.

Proliferative Effect of Aqueous Extract of Sea Cucumber (Holothuria parva) Body Wall on Human Umbilical Cord Mesenchymal Stromal/Stem Cells

“…After sea cucumber extract exposure to MSCs, cyclin D3 increased. Based on the best of our knowledge, no data show the effects of cyclooctaneacetic acid, 2-oxo- on cell proliferation; 8-amino-6-methoxyquinoline has antimalarial and antiplasmodial activity effects [ 52 ]; and 8-quinolinamine analogs did not show any cytotoxicity on cancerous and noncancerous cells [ 53 ]. However, the hematotoxic effect of a metabolite of 8-amino-6-methoxyquinoline on erythrocytes has been reported [ 32 ]; 8-amino-6-methoxyquinoline showed the highest affinity to cyclin D1, cyclin D3, and CDK4.…”