engleski

Synthesis and antiproliferative activity of adamantyl kojic acid derivatives

Kojic acid is a chelating compound and a common fungal metabolite widely used primarily in the preparation of cosmetic biomaterials and skin care products [1]. Numerous studies also showed that kojic acid and its derivatives exhibit other various biological activities [2, 3]. In view of our previous findings on the adamantyl pyridinone derivatives and our continuous investigation of their biological activity [4] we wanted to extend our research further and explore the influence of the adamantyl group on the biological activity of pyranone system as well. Thus, esters of kojic and adamantan‐1‐ylacetic acid were prepared using efficient synthetic methods in good yields and evaluated for their in vitro antiproliferative activity on 4 cancer cell lines (K562, HeLa, Caco‐ 2, NCI‐H358) as well as on normal cells (MDCK). Compounds showed good to moderate in vitro antiproliferative acitvity with IC50 values ranging from 13.1 to 43.0 μM. It seems that the presence and adequate position of the adamantyl acyl group or chlorine atom is a prerequisite for their antitumor activity. The presence and the position of the adamantyl acyl unit were also the important structural parameters that governed antiproliferative activity of our previously investigated pyridin‐4‐ one derivatives.

Kojic acid ; Maltol ; Adamantyl ; Antiproliferation ; Cancer

nije evidentirano