2. Academic Validation
  3. Discovery of tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin KSP

Discovery of tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin KSP

  • Bioorg Med Chem. 2010 Jun 15;18(12):4167-77. doi: 10.1016/j.bmc.2010.05.024.
Fei Liu 1,  Li-Qin Yu,  Cheng Jiang,  Lei Yang,  Wu-Tong Wu,  Qi-Dong You
Affiliations

Affiliation

  • 1 Jiangsu Key Laboratory of Carcinogenesis and Intervention, China Pharmaceutical University, Tongjiaxiang, Nanjing 210009, China.
PMID: 20537544 DOI: 10.1016/j.bmc.2010.05.024
Abstract

Inhibitors of Kinesin spindle protein (KSP) are a promising class of Anticancer agents that cause mitotic arrest in cells from a failure to form functional bipolar mitotic spindles. Here, we report the synthesis and biological evaluation of a novel series of tetrahydro-beta-carboline analogs based on the structure of the known KSP inhibitor HR22C16. Preferred compounds 11b, 12a and 19b were identified as potent inhibitors in a KSP ATPase assay with good anti-proliferative activity in A549 cells.

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