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ChemInform Abstract

Fischer indole synthesis and subsequent aromatization of the B ring of (I) affords the carbazoles (III) in higher yields than the literature route to (IIIb). The structure—activity relationship of the D ring phenyl is conveniently explored via Suzuki couplings on the bromide (IV). Members of the carbazole series are selective for inhibition of the cyclin dependent kinase family of enzymes. Representatives of the series show intra-cdk selectivities, especially for cdk4. Important features of the molecules, responsible for inhibition, are discovered by SAR studies.