2. Academic Validation
  3. 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-κB 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-κB pathway

  • Bioorg Med Chem. 2015 May 1;23(9):2241-6. doi: 10.1016/j.bmc.2015.02.039.
Takashi Misawa 1,  Kosuke Dodo 2,  Minoru Ishikawa 3,  Yuichi Hashimoto 3,  Morihiko Sagawa 4,  Masahiro Kizaki 4,  Hiroshi Aoyama 5
Affiliations

Affiliations

  • 1 Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan; Division of Organic Chemistry, National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya, Tokyo 158-8501, Japan. Electronic address: misawa@nihs.go.jp.
  • 2 Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan; Synthetic Organic Chemistry Laboratory, RIKEN, 2-1 Hirosawa, Wako-shi, Saitama 351-0198, Japan.
  • 3 Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
  • 4 Department of Hematology, Saitama Medical Center, Saitama Medical University, 1981 Kamoda, Kawagoe, Saitama 350-8550, Japan.
  • 5 Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan; School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji-city, Tokyo 192-0392, Japan.
PMID: 25801158 DOI: 10.1016/j.bmc.2015.02.039
Abstract

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, and 18) had inhibitory effects on the growth of multiple myeloma cells (IM-9 cells) by inactivating the NF-κB pathway.

Keywords

1′-Acetoxychavicol acetate (ACA); Benzhydrol skeleton; Multiple myeloma; NF-κB.

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