<p>Twenty novel rupestonic acid amides were designed and synthesized. Their cytotoxic activity was assessed against four human cancer cell lines (HeLa, HT-29, A549, and HepG2). Amide derivative <b>2e</b> exhibited cytotoxic activity against A549 (IC<sub>50</sub> = 4.73 μM) and HT-29 cells (IC<sub>50</sub> = 7.55 μM); <b>1a</b>, against HeLa cells (IC<sub>50</sub> = 13.95 μM); <b>1d</b>, against HepG2 cells (IC<sub>50</sub> = 11.12 μM).</p>

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Design and Synthesis of Rupestonic Acid Derivatives and Assessment of Their Cytotoxic Activity

  • R. Y. Zhu,
  • Kh. Bozorov,
  • H. A. Aisa,
  • J. Y. Zhao

摘要

Twenty novel rupestonic acid amides were designed and synthesized. Their cytotoxic activity was assessed against four human cancer cell lines (HeLa, HT-29, A549, and HepG2). Amide derivative 2e exhibited cytotoxic activity against A549 (IC50 = 4.73 μM) and HT-29 cells (IC50 = 7.55 μM); 1a, against HeLa cells (IC50 = 13.95 μM); 1d, against HepG2 cells (IC50 = 11.12 μM).