Tetrahedron Letters

Novel solid-phase preparation of 2, 6, 9-trisubstituted purines for combinatorial library generation

PH Dorff, RS Garigipati

Index: Dorff, Peter H.; Garigipati, Ravi S. Tetrahedron Letters, 2001 , vol. 42, # 15 p. 2771 - 2773

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Citation Number: 43

Abstract

The purine ring is a critical structural element in several effector molecules (such as agonists, antagonists and substrates) that play a key role in numerous cellular processes. 1., 2., 3. and 4. An example of such an inhibitor is Olomoucine (1), which exhibits a moderate activity (IC 50 =7 μM) towards cdk-2. Despite this moderate activity, the 2,6,9-trisubstituted purine is an ideal scaffold for the generation of kinase inhibitor libraries. Consequently, combinatorial ...