Details

Autor(en) / Beteiligte

• Tsuchiya, Keisuke
• Umeno, Tomohiro
• Tsuji, Genichiro
• Yokoo, Hidetomo
• Tanaka, Masakazu
• Fukuhara, Kiyoshi
• Demizu, Yosuke
• Misawa, Takashi

Titel

Development of Photoswitchable Estrogen Receptor Ligands

Ist Teil von

• Chemical and Pharmaceutical Bulletin, 2020/04/01, Vol.68(4), pp.398-402

Ort / Verlag

Japan: The Pharmaceutical Society of Japan

Erscheinungsjahr

2020

Quelle

MEDLINE

Beschreibungen/Notizen

• Photopharmacology has attracted attention as an approach for the development of novel therapeutics because it allows regulation of the bioactivity of compounds based on their conformational change by photo-irradiation. Previously, we have reported several types of selective estrogen receptor (ER) modulators based on diphenylmethane skeleton. To develop novel photopharmacological reagents, we designed and synthesized a set of ER ligands based on azobenzene skeleton, which can switch its conformation following UV irradiation. Our results showed that after UV irradiation, the Z-form of the synthesized compound 9 interacted with ERα, with a KD value of 2.5 µM, whereas the E-form of compound 9 did not bind ability to ERα at 10 µM.