Cytotoxicity and Antitumor Activity of Arglabin and its Derivatives

BACKGROUND: At present, more than 8000 sesquiterpene lactones have been isolated and described from natural sources, a significant part of which has cytotoxicity antitumor activity. One the practically available is arglabin, which, as renewable material, used for synthesis new compounds. The article presents data on study activity arglabin its derivatives using molecular modeling methods and, in experiment vitro vivo. AIM: aim this work to compounds based lactone experimental pharmacology. METHODS: ChemDraw programs set AutoDock were computer simulation. Molecular docking was carried out Maestro graphical interface Schrödinger Suite software package (Schrödinger, LLC, New York, NY, 2017). Docking modes standard precision XP (extra precision) used. In experiments, compound samples studied models 60 human tumor cell lines, clonogenic C6 rat glioma cells. experiments vivo white outbred rats with transplanted tumors evaluated by inhibition growth magnitude increase average life expectancy. CONCLUSION: When studying lines cells (NCI60), glioma, high some established. connection between structure their inhibitory effect farnesyl protein transferase, topoisomerases -I -II studied.