Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K

…, M Wiesmann, J Chan, S Kaufman, MS Knapp…

Index: Pecchi, Sabina; Ni, Zhi-Jie; Han, Wooseok; Smith, Aaron; Lan, Jiong; Burger, Matthew; Merritt, Hanne; Wiesmann, Marion; Chan, John; Kaufman, Susan; Knapp, Mark S.; Janssen, Johanna; Huh, Kay; Voliva, Charles F. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 16 p. 4652 - 4656

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Citation Number: 2

Abstract

Abstract PI3 kinases are a family of lipid kinases mediating numerous cell processes such as proliferation, migration and differentiation. The PI3 Kinase pathway is often de-regulated in cancer through PI3Kα overexpression, gene amplification, mutations and PTEN phosphatase deletion. PI3K inhibitors represent therefore an attractive therapeutic modality for cancer treatment. Herein we describe how the potency of a benzothiazole fragment hit ...