Synthesis of Novel <i>ent</i>-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells
oleh: Yu Hu, Xiao-Nian Li, Ze-Jin Ma, Pema-Tenzin Puno, Yong Zhao, Yan Zhao, Ye-Zhi Xiao, Wei Zhang, Jing-Ping Liu
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2018-12-01 |
Deskripsi
We have designed and synthesized 6 <i>ent</i>-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 <b>16</b>, <b>17</b> and <b>18</b> 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.