The invention discloses a
toad lactam compound as well as a preparation method and application thereof. The preparation method comprises the steps of: mixing a
toad lactone compound and
ammonium acetate according to
molar ratio of 1: (3-8); dissolving by utilizing
organic solvent; reacting at a temperature of 100-160 DEG C for 0.5-3h under the protection of
inert gas; decompressing, concentrating, removing the
organic solvent; separating and purifying by utilizing a preparative
high performance liquid chromatography method; and obtaining the
toad lactam compound. The preparation method is simple, easy to carry out, safe, reliable and higher in yield. Proved by experiments, the toad
lactam compound obtained in the invention has the advantages of good antitumor effect, very strong inhibitory action on various
cancer cells such as PC3, DU145,
LNCaP, MCF-7 and
Hela, especially much better selective inhibitory action to
hormone-dependent
cancer cells such as the
LNCaP and the MCF-7 than the toad
lactone compound and remarkably lower
toxicity to normal cells than the toad
lactone compound. The toad lactam compound applied in preparing antitumor drugs has the advantages of being high in efficiency and low in
toxicity and meeting the requirements of
drug development.