Synthesis of Novel <i>ent</i>-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells

Abstract

We have designed and synthesized 6 ent-Kaurane-type diterpenoid derivatives containing α,β-unsaturated ketone moieties. In vitro, activity was evaluated against three human tumor cell lines and a rat myogenic cell line (HepG2, NSCLC-H292, SNU-1040, L6) by MTT assay. All the tested compounds exhibited comparable or higher activity than DDP and eriocalyxin B. Compounds 16, 17 and 18 are promising anti-tumor leads due to their cytotoxic potencies and higher selectivity, with SI values of 161.06, 47.80 and 128.20, respectively.

Keywords

• <i>ent</i>-kaurane-type diterpenoid derivatives
• antitumor
• synthesis