title: 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.
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.
authors: 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.
authors: Takashi
authors: T
authors: Misawa
authors: 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.
authors: Kosuke
authors: K
authors: Dodo
authors: Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
authors: Minoru
authors: M
authors: Ishikawa
authors: Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
authors: Yuichi
authors: Y
authors: Hashimoto
authors: Department of Hematology, Saitama Medical Center, Saitama Medical University, 1981 Kamoda, Kawagoe, Saitama 350-8550, Japan.
authors: Morihiko
authors: M
authors: Sagawa
authors: Department of Hematology, Saitama Medical Center, Saitama Medical University, 1981 Kamoda, Kawagoe, Saitama 350-8550, Japan.
authors: Masahiro
authors: M
authors: Kizaki
authors: 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.
authors: Hiroshi
authors: H
authors: Aoyama
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001559:Benzhydryl Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001592:Benzyl Alcohols / Q000737:chemistry*; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D015394:Molecular Structure; D009101:Multiple Myeloma / Q000188:drug therapy* / Q000473:pathology*; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001559:Benzhydryl Compounds; D001592:Benzyl Alcohols; D016328:NF-kappa B; C020225:benzohydrol; C047948:1'-acetoxychavicol acetate
keywords: 1′-Acetoxychavicol acetate (ACA); Benzhydrol skeleton; Multiple myeloma; NF-κB