Practical synthesis of roscovitine and CR8

N Oumata, Y Ferandin, L Meijer…

Index: Oumata, Nassima; Ferandin, Yoan; Meijer, Laurent; Galons, Herve Organic Process Research and Development, 2009 , vol. 13, # 3 p. 641 - 644

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Citation Number: 24

Abstract

Abnormalities in protein phosphorylation have been observed in numerous major human diseases,(1) strongly encouraging the search for pharmacological inhibitors of protein kinases.(2) The 2,6,9-trisubstituted purines were among the first low-molecular weight inhibitors of cyclin-dependent kinases (CDKs).(3) One of these, (R)-roscovitine, 10a (CYC202, Seliciclib), has now reached clinical phase 2 trials against nonsmall cell lung cancer and ...