Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 12, Pages 4167-4177Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.05.024
Keywords
Mitotic kinesin; Inhibitor; Kinesin spindle protein; KSP; Tetrahydro-beta-carboline; Anti-proliferation
Funding
- Natural Science Foundation of China [30772624, 30801437]
- Specialized Research Fund for the Doctoral Program of Higher Education [20060316006, 20090096110003]
- 'The Six Top Talents' of Jiangsu Province [06-C-23]
- National Major Science and Technology Project of China [2008ZX09401-001, 2009ZX09501-003]
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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. (C) 2010 Elsevier Ltd. All rights reserved.
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