title: Design and synthesis of tamoxifen derivatives as a selective estrogen receptor down-regulator.
abstract: We designed and synthesized an estrogen receptor (ER) down-regulator (5), which is a derivative of tamoxifen with a long alkyl side chain. Compound 5 effectively reduced ER protein levels in MCF-7 cells and had an antagonistic effect.
authors: Division of Organic Chemistry, National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan. Electronic address: tsho@nihs.go.jp.
authors: Takuji
authors: T
authors: Shoda
authors: Division of Biochemistry and Molecular Biology, National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan.
authors: Keiichiro
authors: K
authors: Okuhira
authors: Division of Organic Chemistry, National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan; School of Life Sciences, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
authors: Masashi
authors: M
authors: Kato
authors: Division of Organic Chemistry, National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan.
authors: Yosuke
authors: Y
authors: Demizu
authors: School of Life Sciences, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
authors: Hideshi
authors: H
authors: Inoue
authors: Division of Biochemistry and Molecular Biology, National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan.
authors: Mikihiko
authors: M
authors: Naito
authors: Division of Organic Chemistry, National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan; Graduate School of Bioscience and Biotechnology, Tokyo Institute of Technology, 4259 Nagatsuta, Midori-ku, Yokohama, Kanagawa 226-8501, Japan. Electronic address: masaaki@nihs.go.jp.
authors: Masaaki
authors: M
authors: Kurihara
mesh_terms: D004305:Dose-Response Relationship, Drug; D015536:Down-Regulation / Q000187:drug effects; D015195:Drug Design; D006801:Humans; D061986:MCF-7 Cells; D015394:Molecular Structure; D011960:Receptors, Estrogen / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013629:Tamoxifen / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D011960:Receptors, Estrogen; D013629:Tamoxifen
keywords: Breast cancer; Estrogen receptor; SERD; Tamoxifen