Synthesis and biological activity of N-substituted-tetrahydro-γ-carbolines containing peptide residues

• Nadezhda V. Sokolova,
• Valentine G. Nenajdenko,
• Vladimir B. Sokolov,
• Daria V. Vinogradova,
• Elena F. Shevtsova,
• Ludmila G. Dubova and
• Sergey O. Bachurin

Beilstein J. Org. Chem. 2014, 10, 155–162, doi:10.3762/bjoc.10.13

• autooxidation and the t-BHP-induced lipid peroxidation. Keywords: mitochondrial membrane potential; mitochondrial permeability transition; multicomponent; peptides; tetrahydro-γ-carbolines; Ugi multicomponent reaction; Introduction The design and synthesis of new efficient pharmaceutical drugs for the

• diseases [1][2][3]. Thus, one of the specific symptoms of such pathologies is a decrease in the ability of mitochondria to regulate the calcium homeostasis in cells and malfunction of mitochondrial permeability transition (MPT) that represents a key step in the cascades of cell death. From this point of

• membrane potential, mitochondrial permeability transition and lipid peroxidation. Results and Discussion The starting N-substituted tetrahydro-γ-carbolines 3a–d containing a terminal alkyne group were prepared in good yields by heating compounds 1a–d [12][13] with propargyl acrylate (2) in the presence of