Synthesis and evaluation of curcumin derivatives toward an inhibitor of beta-site amyloid precursor protein cleaving enzyme 1

…, K Miyazaki, H Aoki, A Sanjoh, K Kobayashi…

Index: Konno, Hiroyuki; Endo, Hitoshi; Ise, Satomi; Miyazaki, Keiki; Aoki, Hideo; Sanjoh, Akira; Kobayashi, Kazuya; Hattori, Yasunao; Akaji, Kenichi Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 2 p. 685 - 690

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Citation Number: 7

Abstract

Abstract To research a new non-peptidyl inhibitor of beta-site amyloid precursor protein cleaving enzyme 1, we focused on the curcumin framework, two phenolic groups combined with an sp 2 carbon spacer for low-molecular and high lipophilicity. The structure–activity relationship study of curcumin derivatives is described. Our results indicate that phenolic hydroxy groups and an alkenyl spacer are important structural factors for the inhibition of ...