The design and synthesis of purine inhibitors of CDK2. III |
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| Authors: | Shum P W Peet N P Weintraub P M Le T B Zhao Z Barbone F Cashman B Tsay J Dwyer S Loos P C Powers E A Kropp K Wright P S Bitonti A Dumont J Borcherding D R |
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| Institution: | Aventis Pharmaceuticals Inc., Rt. 202-206, Bridgewater, New Jersey 08807, USA. |
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| Abstract: | Cyclin-dependent kinases (CDKs) belong to a class of enzymes that control the ability of a cell to enter into and proceed through the cell division cycle. Using purine as a scaffold, we have synthesized a number of nanomolar inhibitors of CDK-2/cyclin E. In this report, the synthesis of a series of piperidine-substituted purine analogs will be presented, as well as some of their in vitro and in vivo biological effects. |
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