Synthesis of DHDK Derivatives and Study of their Activity

Abstract

AbstractDHDK is a novel diaryl heptanone analog isolated from mistletoe. (1 E, 4 E) 1,7‐bis (4‐hydroxyphenyl) hept‐1,4‐diene‐3‐one (DHDK) exhibits good antitumor activity and excellent stability, but it doesn't have good solubility or bioavailability. In order to improve this deficiency, the structure was modified and five new DHDK derivatives were successfully synthesized. The in vitro cytotoxic activity of DHDK derivatives against four cancer cell lines was determined by Cell Counting Kit‐8 (CCK‐8) assay. The results show that DHDK derivatives exhibit excellent potential, especially for human multiple myeloma cells (KMS‐11) and triple‐negative breast cancer cell line (MDA‐MB 231). The equilibrium solubility and oil‐water partition coefficient of DHDK derivatives were better improved by structural modification.