2. Academic Validation
  3. A chemical platform for the efficient screening of arylazopyrazole-based photoswitchable CENP-E inhibitors using mild cyclization reactions

A chemical platform for the efficient screening of arylazopyrazole-based photoswitchable CENP-E inhibitors using mild cyclization reactions

  • Bioorg Med Chem Lett. 2024 Jul 17:111:129892. doi: 10.1016/j.bmcl.2024.129892.
Kazuya Matsuo 1,  Honoka Ogawa 2,  Shusuke Yamaoka 2,  Tomonori Waku 2,  Akio Kobori 2
Affiliations

Affiliations

  • 1 Faculty of Molecular Chemistry and Engineering, Kyoto Institute of Technology, Matsugasaki, Sakyo-ku, Kyoto 606-8585, Japan. Electronic address: kmatsuo@kit.ac.jp.
  • 2 Faculty of Molecular Chemistry and Engineering, Kyoto Institute of Technology, Matsugasaki, Sakyo-ku, Kyoto 606-8585, Japan.
PMID: 39029538 DOI: 10.1016/j.bmcl.2024.129892
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.

Keywords

Arylazopyrazole; CENP-E; Photopharmacology; Photoswitch.

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