Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.

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Ramurthy S, Subramanian S, Aikawa M, Amiri P, Costales A, Dove J, Fong S, Jansen JM, Levine B, Ma S, McBride CM, Michaelian J, Pick T, Poon DJ, Girish S, Shafer CM, Stuart D, Sung L, Renhowe PA

Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.

J Med Chem. 2008 Nov 27;51(22):7049-52. doi: 10.1021/jm801050k.

PubMed ID

18942827 [ View in PubMed

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Abstract

A series of arylaminobenzimidazoles was designed and synthesized as Raf kinase inhibitors. Exploration of the structure-activity relationship resulted in compounds that are potent in vitro and show desirable in vivo properties.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Sorafenib	RAF proto-oncogene serine/threonine-protein kinase	IC 50 (nM)	1	7.8	22	Details