2,6,9-trisubstituted purines : Optimization towards highly potent and selective CDK1 inhibitors
Novel 2,6,9-substituted purine derivatives represent a class of potent and selective inhibitors of CDK1/cyclinB. The synthesis, SAR and biological profile of selected compounds are described.
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Selective inhibition reveals cyclin-dependent kinase 2 as another kinase that phosphorylates the androgen receptor at serine 81
2018, Biochimica et Biophysica Acta - Molecular Cell ResearchCitation Excerpt :The role of CDK1 in the process of AR phosphorylation has been previously studied using inhibitors with varying degrees of potency towards CDKs, including roscovitine, CGP74514A and RO3306 [12,13,16]. Whereas roscovitine is known to inhibit most CDKs and its suitability as a tool is therefore limited, CGP74514A [27] and RO3306 [28] are sold by many commercial vendors as being specific for CDK1. The CDK selectivity profile of RO3306 has not been published (with the exception of CDK2 and CDK9, which were reported to be poorly sensitive) [29], but targeting CDK1 in cells was observed independently in many studies with different cell types and usually resulted in the blockade of mitosis [30–33] or cyclin B accumulation [28,34].
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