2. Academic Validation
  3. Bis(hetero)aryl derivatives as unique kinesin spindle protein inhibitors

Bis(hetero)aryl derivatives as unique kinesin spindle protein inhibitors

  • Bioorg Med Chem Lett. 2009 Feb 15;19(4):1058-61. doi: 10.1016/j.bmcl.2009.01.018.
Kenji Matsuno 1,  Jun-ichi Sawada,  Mina Sugimoto,  Naohisa Ogo,  Akira Asai
Affiliations

Affiliation

  • 1 Center for Drug Discovery, Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
PMID: 19167222 DOI: 10.1016/j.bmcl.2009.01.018
Abstract

Synthesis of 4-(4-tert-butylphenyl)pyridine analogues as Kinesin spindle protein (KSP) inhibitors, SAR, cytotoxicity and mitotic arrest in HeLa cells are described. Interestingly, PVZB1194 showed potent KSP inhibition only in the presence of microtubules and distinct KSP localization from a known KSP inhibitor S-trytylcysteine analogue in mitosis. The observations would have resulted from a different molecular mechanism of KSP inhibition and suggest a novel biological regulation for KSP in mitosis.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-122247
    99.90%, Kinesin-5 抑制剂
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