Design of Chimeric Histone Deacetylase-and Tyrosine Kinase-Inhibitors: A Series of Imatinib Hybrides as Potent Inhibitors of Wild-Type and Mutant BCR-ABL, PDGF- …

S Mahboobi, S Dove, A Sellmer, M Winkler…

Index: Mahboobi, Siavosh; Dove, Stefan; Sellmer, Andreas; Winkler, Matthias; Eichhorn, Emerich; Pongratz, Herwig; Ciossek, Thomas; Baer, Thomas; Maier, Thomas; Beckers, Thomas Journal of Medicinal Chemistry, 2009 , vol. 52, # 8 p. 2265 - 2279

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Citation Number: 58

Abstract

Inhibitors of histone deacetylases are a new class of cancer therapeutics with possibly broad applicability. Combinations of HDAC inhibitors with the kinase inhibitor 1 (Imatinib) in recent studies showed additive and synergistic effects. Here we present a new concept by combining inhibition of protein kinases and HDACs, two independent pharmacological activities, in one synthetic small molecule. In general, the HDAC inhibition profile, the ...