Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1363726 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
This Letter describes the discovery and key structure-activity relationship (SAR) of a series of 2-aminobenzimidazoles as potent Aurora kinase inhibitors. 2-Aminobenzimidazole serves as a bioisostere of the biaryl urea residue of SNS-314 (1c), which is a potent Aurora kinase inhibitor and entered clinical testing in patients with solid tumors. Compared to SNS-314, this series of compounds offers better aqueous solubility while retaining comparable in vitro potency in biochemical and cell-based assays; in particular, 6m has also demonstrated a comparable mouse iv PK profile to SNS-314.
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Authors
Min Zhong, Minna Bui, Wang Shen, Subramanian Baskaran, Darin A. Allen, Robert A. Elling, W. Michael Flanagan, Amy D. Fung, Emily J. Hanan, Shannon O. Harris, Stacey A. Heumann, Ute Hoch, Sheryl N. Ivy, Jeffrey W. Jacobs, Stuart Lam, Heman Lee,