This invention relates to the preparation of 10-trifluoromethoxycamptothecin compounds and their use in antitumor drugs. The
structural formula of these compounds is shown below.
In vitro cytotoxicity screening results show that 10-trifluoromethoxycamptothecin compounds possess broad-spectrum
antitumor activity, exhibiting strong inhibitory activity against human
hepatocellular carcinoma cells (HepG2), human non-
small cell lung cancer cells (A549),
human colon cancer cells (SW480), human cholangiocarcinoma cells (QBC939),
human breast cancer cells (MCF-7), human
pancreatic cancer cells (PANC-1), and human
pancreatic cancer cells (BxPC-3). Compounds 10-trifluoromethoxycamptothecin I and 7-ethyl-10-trifluoromethoxycamptothecin II showed strong inhibitory effects against all seven tested tumor
cell lines, with IC50 values exceeding 100%. 50 The concentrations were 0.913–0.0661 μM and 4.932–0.0578 μM, respectively, both significantly superior to the control
drug topotecan. Among them, compounds I and II exhibited the strongest inhibitory activity against the BxPC-3
cell line, with IC50 values of [missing value]. 50 The values were 0.0661±0.0065μM and 0.0578±0.0043μM, respectively. Therefore, 10-trifluoromethoxycamptothecin compounds hold promise for development into a novel antitumor
drug.