Baicalin and its aglycone baicalein derived from Scutellaria baicalensis exhibited potent anticancer effects in various types of cancer cell lines. However, the unfavorable pharmaceutical properties became the main obstacle for their potential clinical development. With the aim of development of novel anticancer agents based on the skeleton of baicalin, a series of novel negletein derivatives were designed and synthesized. Among them, compound 8 (FZU‐02,006) with an N,N‐dimethylamino ethoxyl moiety at the C‐6 position exhibited significant enhanced antiproliferative effect against HL‐60 cells in vitro through regulating multisignaling pathways. These results revealed that compound 8 with the improved aqueous solubility (as HCl salt, >1 mg/ml) and enhanced antileukemia potency might serve as a promising lead for further development.

中文翻译：

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发现新的神经钙蛋白衍生物作为急性髓细胞白血病的有效抗癌药

来自黄S的黄a苷及其苷元黄ical苷在各种类型的癌细胞系中均显示出有效的抗癌作用。然而，不利的药物特性成为其潜在临床开发的主要障碍。为了开发基于黄ical苷骨架的新型抗癌药，设计并合成了一系列新型神经钙蛋白衍生物。其中，在C-6位置具有N，N-二甲基氨基乙氧基部分的化合物8（FZU- 02,006）通过调节多信号通路，在体外对HL-60细胞具有显着增强的抗增殖作用。这些结果表明，化合物8 具有改善的水溶性（如HCl盐，> 1 mg / ml）和增强的抗白血病能力可能是进一步开发的有希望的线索。