Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP |
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| Authors: | Fraley Mark E Garbaccio Robert M Arrington Kenneth L Hoffman William F Tasber Edward S Coleman Paul J Buser Carolyn A Walsh Eileen S Hamilton Kelly Fernandes Christine Schaber Michael D Lobell Robert B Tao Weikang South Victoria J Yan Youwei Kuo Lawrence C Prueksaritanont Thomayant Shu Cathy Torrent Maricel Heimbrook David C Kohl Nancy E Huber Hans E Hartman George D |
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| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. mark_fraley@merck.com |
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| Abstract: | 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<10nM. Ancillary hERG activity was evaluated for this series of inhibitors. |
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