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Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR. | LitMetric
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Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR.

Mark T Bilodeau April M Cunningham Timothy J Koester Patrice A Ciecko Kathleen E Coll William R Huckle Randall W Hungate Richard L Kendall Rosemary C McFall Xianzhi Mao Ruth Z Rutledge Kenneth A Thomas

Bioorg Med Chem Lett

Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA.

Published: August 2003

1,5-Diarylbenzimidazoles have been identified as potent inhibitors of KDR kinase activity. The series was developed with a goal of finding compounds with optimal drug-like properties. This communication describes structural modifications in the series that enhance solubility, lower protein binding, and provide compounds with excellent potency and pharmacokinetic profiles.

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 Source
http://dx.doi.org/10.1016/s0960-894x(03)00485-2DOI Listing

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