Targeting the PPM1D phenotype; 2,4-bisarylthiazoles cause highly selective apoptosis in PPM1D amplified cell-lines

The metal-dependent phosphatase PPM1D (WIP1) is an important oncogene in cancer, with over-expression of the protein being associated with significantly worse clinical outcomes. In this communication we describe the discovery and optimization of novel 2,4-bisarylthiazoles that phenocopy the knockdow...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-08, Vol.24 (15), p.3469-3474
Hauptverfasser:	Cheeseman, Matthew D, Faisal, Amir, Rayter, Sydonia, Barbeau, Olivier R, Kalusa, Andrew, Westlake, Maura, Burke, Rosemary, Swan, Michael, van Montfort, Rob, Linardopoulos, Spiros, Jones, Keith
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Apoptosis - drug effects Cell Line, Tumor Cell Proliferation - drug effects Dose-Response Relationship, Drug Drug Discovery Drug Screening Assays, Antitumor Humans Molecular Structure Phenotype Phosphoprotein Phosphatases - antagonists & inhibitors Phosphoprotein Phosphatases - metabolism Protein Phosphatase 2C Structure-Activity Relationship Thiazoles - chemical synthesis Thiazoles - chemistry Thiazoles - pharmacology Tumor Suppressor Protein p53 - metabolism
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