Abstract

Despite disappointing results with the Raf inhibitor ZM 336372, AstraZeneca claims new B-Raf kinase inhibitors with the same m-phenylenediamine core structure. The new bisamides have two distinct linker groups attached. One is a substituted aromatic carboxylic acid group that constitutes the lipophilic part of the molecule, and the other is usually a pyrimidine carboxylic acid. The new molecules are part of a series of m-phenylenediamine bisamides. The compounds are expected to have anticancer activity due to their B-Raf inhibitory activity. B-Raf is mutated in a number of cancers into a constitutively active enzyme.

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