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Novel caffeine derivatives with antiproliferative activity

机译：具有抗增殖活性的新型咖啡因衍生物

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摘要

Caffeine is probably the best known and most widely used psychoactive substance in the world. Beside its psychoactive effects, caffeine has been found to affect the cell cycle and DNA repair, as a consequence of the inhibition of ATM and ATR kinases. These two DNA damage response kinases, members of the phosphatidylinositol 3-kinase related protein kinase family, represent very attractive anticancer drug targets. Their inhibition can selectively sensitize cancer cells to DNA damaging agents and even kill various tumour cells in monotherapy. We developed a series of caffeine derivatives and evaluated their antiproliferative effects on 11 human tumour cell lines and compared them against caffeine and a standard ATR inhibitor VE-821. Although the new caffeine derivatives did not achieve the overall potency of VE-821, several compounds exhibited enhanced antiproliferative activity compared to caffeine and in some cell lines showed at least comparable activity to VE-821.
机译：咖啡因可能是世界上最知名，使用最广泛的精神活性物质。除了抑制精神活性外，还发现咖啡因会抑制ATM和ATR激酶，从而影响细胞周期和DNA修复。这两个DNA损伤反应激酶是磷脂酰肌醇3-激酶相关蛋白激酶家族的成员，代表了非常有吸引力的抗癌药物靶标。它们的抑制作用可以选择性地使癌细胞对DNA破坏剂敏感，甚至可以在单一疗法中杀死各种肿瘤细胞。我们开发了一系列咖啡因衍生物，并评估了它们对11种人类肿瘤细胞系的抗增殖作用，并将它们与咖啡因和标准ATR抑制剂VE-821进行了比较。尽管新的咖啡因衍生物不能达到VE-821的整体功效，但与咖啡因相比，几种化合物显示出增强的抗增殖活性，并且在某些细胞系中显示出至少与VE-821相当的活性。

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