H. M. Chen, Mei‐Hua Hsu, Li‐Jiau Huang, J. Chung, Hung-Yi Chen, F. Lung, C. Hung, M. Liau, S. Kuo
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引用次数: 0
Abstract
A series of N-phenylacetyl-D-amino acid derivatives were prepared and tested against HL-60 cells for differentiation and antiproliferation activities. Among them, five compounds, phenylacetyl-D-valine (17), phenylacetyl-D-leucine (18), phenylacetyl-D-Isoleucine (19), phenylacetyl-D-phenylalanine (21) and phenylacetyl-D-phenylglycine (22) were found to significantly potentiate the all-trans retinoic acid (ATRA)-induced differentiation. The three most effective compounds, 17, 18, and 19 were investigated to ascertain their effects on the cell cycle and were found to behave like ATRA in prohibiting the entry into S phase and G2/M phase. Our findings suggest that when administered together with ATRA, compounds 17, 18, and 19 may have therapeutically beneficial effect in the treatment of acute promyelocytic leukemia (APL).
制备了一系列n -苯基乙酰- d -氨基酸衍生物，并对HL-60细胞进行了分化和抗增殖活性试验。其中，苯乙酰基- d -缬氨酸(17)、苯乙酰基- d -亮氨酸(18)、苯乙酰基- d -异亮氨酸(19)、苯乙酰基- d -苯丙氨酸(21)和苯乙酰基- d -苯甘氨酸(22)5种化合物能显著增强全反式维甲酸(ATRA)诱导的分化。研究了三种最有效的化合物17、18和19，以确定它们对细胞周期的影响，发现它们的行为与ATRA类似，可以阻止细胞进入S期和G2/M期。我们的研究结果表明，当与ATRA一起使用时，化合物17、18和19可能对治疗急性早幼粒细胞白血病(APL)具有有益的治疗效果。
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