In an attempt to search for new natural product-based antitumor agents, a series of novel (aryl)methyl-amine derivatives of dehydroabietic acid-based B ring-fused-thiazole were designed and synthesized. The primary bioassay showed that compounds 5r and 5s presented certain inhibitory activity against cancer cells, weak cytotoxic activity against normal cells, and inhibitory activity against PI3K/AKT/mTOR signaling pathway. The binding modes and the binding site interactions between the active compounds and the target proteins were predicted preliminarily by the molecular docking method.

中文翻译：

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基于脱氢枞酸的 B 环稠合噻唑的（芳基）甲基胺衍生物作为潜在 PI3K/AKT/mTOR 信号通路抑制剂的合成和抗肿瘤评价。

为了寻找新的基于天然产物的抗肿瘤剂，设计并合成了一系列基于脱氢枞酸的新型（芳基）甲基胺衍生物 B 环稠合噻唑。初步生物测定表明，化合物5r和5s对癌细胞具有一定的抑制活性，对正常细胞的细胞毒活性较弱，对PI3K/AKT/mTOR信号通路具有抑制活性。采用分子对接法初步预测了活性化合物与靶蛋白的结合方式和结合位点相互作用。