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<p>In this study, 20 tetrahydroisoquinoline (THIQ)-NO donor hybrids, derived from our in-house trans-<i>β</i>-arylacryl-THIQ-based scaffold, were designed, synthesized, and in vitro biologically evaluated as potential anti-cancer therapeutics. Among them, compounds <b>13h</b>, <b>j</b> and <b>20b</b> exerted anti-proliferative activities at single-digit micromolar level against A549, HepG2, HCT-116, and HL-60 cell lines, which are superior to those of the parent compound <b>7</b>. The anti-proliferative potency of <b>13j</b> and <b>20g</b> against HL-60 cells were comparable to that of gefitinib. In addition, <b>13j</b> induced the release of NO in HepG2 cells in a dose-dependent manner. The western blot analysis illustrated that <b>13j</b> also dose-dependently ablated the phosphorylation of AKT and ERK1/2 in this cell line. With the aforementioned attractive performance, compound <b>13j</b> deserves further functional investigation.</p>

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Discovery of structurally novel tetrahydroisoquinoline derivatives bearing NO donor as potential anti-cancer therapeutics

  • 期刊论文

  • 发表日期：

    2025年3月26日

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  • Hao Chen,
  • Xin Gao,
  • Siqi Fan,
  • Xiaodong Ma,
  • Fang Fang

摘要

In this study, 20 tetrahydroisoquinoline (THIQ)-NO donor hybrids, derived from our in-house trans-β-arylacryl-THIQ-based scaffold, were designed, synthesized, and in vitro biologically evaluated as potential anti-cancer therapeutics. Among them, compounds 13h, j and 20b exerted anti-proliferative activities at single-digit micromolar level against A549, HepG2, HCT-116, and HL-60 cell lines, which are superior to those of the parent compound 7. The anti-proliferative potency of 13j and 20g against HL-60 cells were comparable to that of gefitinib. In addition, 13j induced the release of NO in HepG2 cells in a dose-dependent manner. The western blot analysis illustrated that 13j also dose-dependently ablated the phosphorylation of AKT and ERK1/2 in this cell line. With the aforementioned attractive performance, compound 13j deserves further functional investigation.