Structure-Activity Relationships of Benzhydrol Derivatives Based on 1'-Acetoxychavicol Acetate (ACA) and their Inhibitory Activities on Multiple Myeloma Cell Growth via Inactivation of the NF-kB Pathway

Structure-Activity Relationships of Benzhydrol Derivatives Based on 1'-Acetoxychavicol Acetate (ACA) and their Inhibitory Activities on Multiple Myeloma Cell Growth via Inactivation of the NF-kB Pathway
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基于 1-Acetoxychavicol Acetate (ACA) 的苯甲醇衍生物的构效关系及其通过 NF-kB 通路失活对多发性骨髓瘤细胞生长的抑制活性

DOI:
10.1016/j.bmc.2015.02.039
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发表时间:
2015
影响因子:
3.5
通讯作者:
Hiroshi Aoyama
Hiroshi Aoyama
中科院分区:
医学3区
文献类型:
--
作者:
Takashi Misawa;Kosuke Dodo;Minoru Ishikawa;Yuichi Hashimoto;Morihiko Sagawa;Masahiro Kizaki;Hiroshi Aoyama

文献摘要

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1′-乙酰氧基胡椒酚乙酸酯(ACA)是从菊科植物根茎中分离得到的一种具有抗炎、抗人类免疫缺陷病毒(HIV)和抗癌等多种生物活性的化合物。ACA是治疗许多癌症的有吸引力的候选药物。本文研究了基于二苯甲醇骨架的ACA衍生物在人白血病细胞(HL-60)中的构效关系。结果表明,所合成的ACA衍生物(ACA,1和18)通过抑制NF-κB通路抑制多发性骨髓瘤细胞(IM-9)的生长。
1′-Acetoxychavicol acetate (ACA), which was isolated from the rhizomes of Zingiberaceae, exhibits various biological actions, including anti-inflammatory, anti-human immunodeficiency virus (HIV), and anti-cancer activities. ACA represents an attractive candidate for the treatment of many cancers. We herein examined the structure–activity relationships of ACA derivatives based on the benzhydrol skeleton in human leukemia cells (HL-60). Our results revealed that the ACA derivatives synthesized (ACA,1, and18) had inhibitory effects on the growth of multiple myeloma cells (IM-9 cells) by inactivating the NF-κB pathway.