Synthesis of novel noscapine triazole tethered derivatives with γ-aminobutyric acid (GABA) linker is reported. Attachment of the linker was done by N-demethylation of noscapine followed by coupling with N-Boc protected GABA. The straightforward synthesis of the target molecules was made by a three-component reaction between GABA-noscapine, p-nitrophenyl azide, and commercially available ketones under metal-free conditions to produce a library with diverse functional groups. Anticancer activity of the synthesized derivatives was evaluated on MCF-7 cancer cell line. The best anticancer activity was demonstrated by a compound with an IC₅₀ value of 57.2 µM, close to that of noscapine (IC₅₀ = 55.2 µM).

Graphical abstract

中文翻译：

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Noscapine 新型 GABA-三唑系衍生物的合成及其抗癌活性

报道了带有γ-氨基丁酸 (GABA) 连接体的新型诺斯卡品三唑系衍生物的合成。通过诺斯卡品的N-去甲基化，然后与N -Boc 保护的 GABA 偶联来完成接头的连接。目标分子的直接合成是通过 GABA-那斯卡品、对硝基苯基叠氮化物和市售酮在无金属条件下的三组分反应来产生具有不同官能团的文库。在 MCF-7 癌细胞系上评估了合成衍生物的抗癌活性。_{最佳抗癌活性是由 IC 50}值为 57.2 µM的化合物证明的，接近诺斯卡品 (IC ₅₀  = 55.2 µM)。

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