New effective inhibitors of the Abelson kinase

…, M Mokhtarian, S Mehanovic, M Nilsen-Hamilton

Index: Kraus, George A.; Gupta, Vinayak; Mokhtarian, Marjan; Mehanovic, Samir; Nilsen-Hamilton, Marit Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 17 p. 6316 - 6321

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Citation Number: 6

Abstract

The effects of substituents on the aryl ring were studied by the preparation and testing of several PD173955 analogs. Inserting a single carbon atom into the C–N bond in the aniline subunit (PDC) reduced the kinase inhibition by a factor of 200. Despite its decreased affinity for Abl compared with PD173955, PDC exhibits a Ki very similar to that reported for Imatinib. Increased water solubility is also gained by replacing the thiomethyl group with an amino ...