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Communication | Special issue | Vol 101, No. 2, 2020, pp.429-434
Published online, 29th August, 2019
DOI: 10.3987/COM-19-14121
Design and Synthesis of 4-(2-Pyrrolyl)-4-phenylheptane Derivatives as Estrogen Receptor Antagonists

Miyako Naganuma, Hidetomo Yokoo, Takashi Misawa, Kenji Matsuno, Genichiro Tsuji,* and Yosuke Demizu*

*Division of organic chemistry, National Institute of Hygienic Sciences, 3-25-26, Tonomachi, Kawasaki-ku, Kawasaki-shi, Kanagawa 210-9501, Japan

Abstract

The estrogen receptor (ER) has been recognized as a potential target for the treatment of breast cancer, which is the most common malignancy found in woman. In this study, a series of 4-(2-pyrrolyl)-4-phenylheptane derivatives as ER antagonists were designed and synthesized. The ER antagonistic activity of these compounds was evaluated to study their structure-activity relationships.