2. Academic Validation
  3. Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity

Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity

  • Bioorg Med Chem. 2011 Sep 15;19(18):5446-53. doi: 10.1016/j.bmc.2011.07.054.
Delany Rodriguez 1,  Chinnasamy Ramesh,  Lauren H Henson,  Lori Wilmeth,  Bj K Bryant,  Samuel Kadavakollu,  Rebecca Hirsch,  Johnelle Montoya,  Porsha R Howell,  Jon M George,  David Alexander,  Dennis L Johnson,  Jeffrey B Arterburn,  Charles B Shuster
Affiliations

Affiliation

  • 1 Department of Biology, New Mexico State University, Las Cruces, NM 88003, USA.
PMID: 21855351 DOI: 10.1016/j.bmc.2011.07.054
Abstract

Assembly of a bipolar mitotic spindle requires the action of class 5 kinesins, and inhibition or depletion of this motor results in mitotic arrest and Apoptosis. S-Trityl-l-cysteine is an allosteric inhibitor of vertebrate Kinesin Spindle Protein (KSP) that has generated considerable interest due to its anti-cancer properties, however, poor pharmacological properties have limited the use of this compound. We have modified the triphenylmethyl and cysteine groups, guided by biochemical and cell-based assays, to yield new cysteinol and cysteamine derivatives with increased inhibitory activity, greater efficacy in model systems, and significantly enhanced potency against the NCI60 tumor panel. These results reveal a promising new class of conformationally-flexible small molecules as allosteric KSP inhibitors for use as research tools, with activities that provide impetus for further development as anti-tumor agents.

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