DAAS is the diacetoxy acetal derivative of a-santonin and induces HL-60 cell differentiation into granulocytes. In this report, we investigated the structure-activity relationship (SAR) of DAAS derivatives in the differentiation of human HL-60 leukemia cells. Although its derivatives themselves had less effect on HL-60 cell differentiation than DAAS, the monoacetyl derivative, 2, mainly induced HL-60 cell differentiation. Moreover, compound 2 synergistically enhanced all-trans retinoic acid (ATRA)-induced HL-60 cell differentiation when combined with 50 nM ATRA, a well-known differentiation inducer. This enhancing effect is similar to that of DAAS in ATRA-induced differentiation.

译文

:DAAS是α-桑顿宁的二乙酰氧基乙缩醛衍生物,可诱导HL-60细胞分化为粒细胞。在本报告中,我们研究了DAAS衍生物在人HL-60白血病细胞分化中的构效关系(SAR)。尽管其衍生物本身对HL-60细胞分化的影响小于DAAS,但一元乙酰衍生物2主要诱导HL-60细胞分化。此外,当与众所周知的分化诱导剂50 nM ATRA联合使用时,化合物2协同增强了全反式维甲酸(ATRA)诱导的HL-60细胞分化。在ATRA诱导的分化中,这种增强作用与DAAS相似。

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