Synthesis and anticancer activity of podophyllotoxin derivatives with nitrogen-containing heterocycles.

ABSTRACT: Three series of podophyllotoxin derivatives with various nitrogen-containing heterocycles were designed and synthesized. The antitumor activity of these podophyllotoxin derivatives was evaluated in vitro against a panel of human tumor cell lines. The results showed that podophyllotoxin-imidazolium salts and podophyllotoxin-1,2,4-triazolium salts a1-a20 exhibited excellent cytotoxic activity. Among them, a6 was the most potent cytotoxic compound with IC₅₀ values of 0.04-0.29 μM. Podophyllotoxin-1,2,3-triazole derivatives b1-b5 displayed medium cytotoxic activity, and podophyllotoxin-amine compounds c1-c3 has good cytotoxic activity with IC₅₀ value of 0.04-0.58 μM. Furthermore, cell cycle and apoptosis experiments of compound a6

SUBMITTER: Yin M 

PROVIDER: S-EPMC10206303 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature