Solid-phase synthesis and anticancer activity of diarylheptanoid amide derivatives

Abstract

A library of diarylheptanoid amide derivatives were synthesized by solid-phase synthesis technique using reusable linker. Diarylheptanoid amide derivatives obtained were screened for cytotoxicity activity against cancer and normal cell lines. 4-Chlorobenzoyl analogues exhibited moderate activity against human colon adenocarcinoma cell line (HT29) and human breast adenocarcinoma cell line (MCF-7) with IC₅₀ values of 38.61 and 40.15 µg/ml, respectively. Moreover, 4-chlorobenzoyl analogues showed no cytotoxic activity against the normal cell (HEK293) with IC₅₀ value of 747.20 µg/ml. The selectivity index value of 4-chlorobenzoyl analogues was greater than that of doxorubicin and curcumin.