Synthesis and in vitro biological evaluation of 2, 6, 9-trisubstituted purines targeting multiple cyclin-dependent kinases

…, T Gucký, E Řezníčková, J Voller, T Pospíšil…

Index: Zatloukal, Marek; Jorda, Radek; Gucky, Tomas; Reznickova, Eva; Voller, Jiri; Pospisil, Tomas; Malinkova, Veronika; Adamcova, Helena; Krystof, Vladimir; Strnad, Miroslav European Journal of Medicinal Chemistry, 2013 , vol. 61, p. 61 - 72

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Citation Number: 18

Abstract

Several inhibitors of cyclin-dependent kinases (CDKs), including the 2, 6, 9-trisubstituted purine derivative roscovitine, are currently being evaluated in clinical trials as potential anticancer drugs. Here, we describe a new series of roscovitine derivatives that show increased potency in vitro. The series was tested for cytotoxicity against six cancer cell lines and for inhibition of CDKs. For series bearing 2-(hydroxyalkylamino) moiety, cytotoxic ...