Synthesis and Antitumor Activities of Phenanthrene-Based Alkaloids

A series of phenanthrene-based tylophorine derivatives (PBTs) were synthesized and their cytotoxic activities against the H460 human large-cell lung carcinoma cell line were evaluated. Among these compounds, N-(3-hydroxy-2,6,7-tri-methoxyphenanthr-9-ylmethyl)-L-prolinol (5a), and N-(3-hydroxy-2,6,7-trimethoxy-phenanthr-9-ylmethyl)-L-valinol (9) exhibited good activities, with IC50 values of 11.6 and 6.1 mM, respectively