<p>Twenty-seven asiatic acid derivatives were designed and synthesized in this paper, including twenty-two new compounds. The synthesized compounds were confirmed by <sup>1</sup>H NMR, <sup>13</sup>C NMR and HRMS. The antitumor activities of all compounds against A549, Hela and HepG2 cancer cells in vitro were evaluated. Notably, <b>AA-6a</b> (IC<sub>50</sub> = 1.10 ± 0.25 μM) has better antitumor activity than gefitinib (IC<sub>50</sub> = 83.75 ± 1.72 μM) against A549 cells. <b>AA-6b</b> (IC<sub>50</sub> = 2.38 ± 0.36 μM) has better antitumor activity than gefitinib (IC<sub>50</sub> = 33.88 ± 1.51 μM) on Hela cells. <b>AA-2b</b> (IC<sub>50</sub> = 1.55 ± 0.21 μM) has the better antitumor activity than gefitinib (IC<sub>50</sub> = 48.37 ± 1.07 μM) against HepG2 cells.</p><p></p>

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Synthesis, characterization and in vitro antitumor activity of asiatic acid derivatives

  • Panpan Wang,
  • Jie Liu,
  • Lantian Cui,
  • Gao Li,
  • Longxuan Zhao,
  • Mei Jin

摘要

Twenty-seven asiatic acid derivatives were designed and synthesized in this paper, including twenty-two new compounds. The synthesized compounds were confirmed by 1H NMR, 13C NMR and HRMS. The antitumor activities of all compounds against A549, Hela and HepG2 cancer cells in vitro were evaluated. Notably, AA-6a (IC50 = 1.10 ± 0.25 μM) has better antitumor activity than gefitinib (IC50 = 83.75 ± 1.72 μM) against A549 cells. AA-6b (IC50 = 2.38 ± 0.36 μM) has better antitumor activity than gefitinib (IC50 = 33.88 ± 1.51 μM) on Hela cells. AA-2b (IC50 = 1.55 ± 0.21 μM) has the better antitumor activity than gefitinib (IC50 = 48.37 ± 1.07 μM) against HepG2 cells.