Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 16, Issue 7, Pages 1775-1779Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.01.030
Keywords
KSP; hERG; dihydropyrroles; kinesin spindle protein; antimitotics; antiproliferative; anticancer
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The evolution of 2,4-diaryl-2,5-dihydropyrroles as inhibitors of KSP is described. Introduction of basic amide and urea moieties to the dihydropyrrole nucleus enhanced potency and aqueous solubility, simultaneously, and provided compounds that caused mitotic arrest of A2780 human ovarian carcinoma cells with EC(50)s < 10 nM. Ancillary hERG activity was evaluated for this series of inhibitors. (C) 2006 Elsevier Ltd. All rights reserved.
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