Itk kinase inhibitors: Initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead

…, M Winters, L Qiao, D Ryan, R DesJarlis…

Index: Moriarty, Kevin J.; Winters, Michael; Qiao, Lei; Ryan, Declan; DesJarlis, Renee; Robinson, Darius; Cook, Brian N.; Kashem, Mohammed A.; Kaplita, Paul V.; Liu, Lisa H.; Farrell, Thomas M.; Khine, Hnin Hnin; King, Josephine; Pullen, Steven S.; Roth, Gregory P.; Magolda, Ronald; Takahashi, Hidenori Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 20 p. 5537 - 5540

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Citation Number: 21

Abstract

Previously, we reported a series of novel benzimidazole based Itk inhibitors that exhibited excellent enzymatic potency and selectivity but low microsomal stability. Employing a structure based approach a new series of inhibitors with comparable potency and selectivity to the original series and with a potential for improved microsome stability was identified.