In order to assess traditional claims about the therapeutic potential of Caucasian endemic medicinal plants and to select plants for phytochemical research, nine plant species were selected and assessed for their in-vitro antioxidant and cytotoxic activities. The metabolite profiles of some priority plants were analysed.Antioxidant effects were assessed using the 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) system, lipid peroxidation and Folin-Ciocalteu methods. Cytotoxic activities were examined against human liver cancer cells (HepG2) using the Alamar Blue assay. Terpenoids of selected species were analysed by GC and GC-MS. Polyphenols were separated by HPLC.Thymus transcaucasicus, Heracleum transcaucasicum, Ribes armenum, Crataegus armena showed most promising antioxidant activity in ABTS model system. Moreover, Rubus takhtadjanii, C. armena, T. transcaucasicus showed a high level of antioxidant activity by inhibiting lipid peroxidation. C. armena and T. transcaucasicus expressed high-to-moderate cytotoxicity against HepG2 cells. The main terpenoids and polyphenols of Centaurea hajastana, C. armena and T. transcaucasicus were quantified.This study provides in-vitro data relevant for assessing the use of Caucasian endemic medicinal plants, most importantly C. armena and T. transcaucasicus as traditional antioxidant supplements and potential anticancer remedies. Metabolite profiles of some lead plants showed the nature of bioactive compounds of medical interest.