Medicinal Chemistry

Solid-Phase Synthesis and In Vitro Cytotoxicity of New Peptide Functionalized Cyclencarboxymethylen and L-DOPA Hybrids

Abstract

L Arabuli, R Jezek, T Macek, P Lovecka, E Nikoleishvili, N Sulashvili and I Maisuradze

The new small peptide functionalized cyclen and DOPA derivatives were synthesized: cyclen-HisHis, cyclen- AspHis, cyclen-GluHis, DOPA-HisHis were prepared. The solid-phase synthesis strategy was used for preparation of new compounds. Synthesized cyclen- and DOPA-oligopeptide hybrid conjugations were purified by HPLC and analyzed using MALDI-TOF MS spectrometer. The toxic effect was determined against mammalian cells human embryonic kidney cell line HEK293T ATCC®CLR-11268TM for each new compound. The inhibition effect of all tested cyclen– dipeptides on kidney cells was approximately about 30% after 24 hours. The minimal rate of toxicity against human liver cells showed all tested dipeptides with DOPA, their inhibition effect was maximal 10%. The acute inhibition effect of sample DOPA-GluHis-DOPA was 14% imme¬diately after adding. The antioxidant and anticancer activity studies will be next part of the ongoing project.