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A chemical platform for the efficient screening of arylazopyrazole-based photoswitchable CENP-E inhibitors using mild cyclization reactions.
Matsuo, Kazuya; Ogawa, Honoka; Yamaoka, Shusuke; Waku, Tomonori; Kobori, Akio.
Affiliation
  • Matsuo K; Faculty of Molecular Chemistry and Engineering, Kyoto Institute of Technology, Matsugasaki, Sakyo-ku, Kyoto 606-8585, Japan. Electronic address: kmatsuo@kit.ac.jp.
  • Ogawa H; Faculty of Molecular Chemistry and Engineering, Kyoto Institute of Technology, Matsugasaki, Sakyo-ku, Kyoto 606-8585, Japan.
  • Yamaoka S; Faculty of Molecular Chemistry and Engineering, Kyoto Institute of Technology, Matsugasaki, Sakyo-ku, Kyoto 606-8585, Japan.
  • Waku T; Faculty of Molecular Chemistry and Engineering, Kyoto Institute of Technology, Matsugasaki, Sakyo-ku, Kyoto 606-8585, Japan.
  • Kobori A; Faculty of Molecular Chemistry and Engineering, Kyoto Institute of Technology, Matsugasaki, Sakyo-ku, Kyoto 606-8585, Japan.
Bioorg Med Chem Lett ; 111: 129892, 2024 Oct 01.
Article in En | MEDLINE | ID: mdl-39029538
ABSTRACT
A set of arylazopyrazole-based inhibitors targeting the mitotic motor protein CENP-E was discovered through the chemical platform using the quantitative cyclization of 1,3-diketone intermediate with various hydrazines under mild conditions. Through this efficient platform, the structure-activity relationship pertaining to the pyrazole photoswitch in photoswitchable CENP-E inhibitors not only in vitro but also in cells was successfully clarified.
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Full text: 1 Database: MEDLINE Main subject: Pyrazoles / Chromosomal Proteins, Non-Histone Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2024 Type: Article
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Full text: 1 Database: MEDLINE Main subject: Pyrazoles / Chromosomal Proteins, Non-Histone Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2024 Type: Article