Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors

Design and optimization of novel imidazopyridine derivatives led to the identification of a potent and selective PLK inhibitor 36. A novel class of imidazopyridine derivatives was designed as PLK1 inhibitors. Extensive SAR studies supported by molecular modeling afforded a highly potent and selectiv...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-08, Vol.19 (16), p.4673-4678
Hauptverfasser:	Sato, Yoshiyuki, Onozaki, Yu, Sugimoto, Tetsuya, Kurihara, Hideki, Kamijo, Kaori, Kadowaki, Chie, Tsujino, Toshiaki, Watanabe, Akiko, Otsuki, Sachie, Mitsuya, Morihiro, Iida, Masato, Haze, Kyosuke, Machida, Takumitsu, Nakatsuru, Yoko, Komatani, Hideya, Kotani, Hidehito, Iwasawa, Yoshikazu
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Cell Cycle Proteins - antagonists & inhibitors Cell Cycle Proteins - metabolism Cell Line, Tumor Computer Simulation General aspects HeLa Cells Humans Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - pharmacology Imidazopyridine Medical sciences Models, Chemical Pharmacology. Drug treatments PLK1 Polo-like kinase Polo-Like Kinase 1 Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein Serine-Threonine Kinases - antagonists & inhibitors Protein Serine-Threonine Kinases - metabolism Proto-Oncogene Proteins - antagonists & inhibitors Proto-Oncogene Proteins - metabolism Pyridines - chemical synthesis Pyridines - chemistry Pyridines - pharmacology Rats Structure-Activity Relationship Xenograft Model Antitumor Assays
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Beschreibung
Zusammenfassung:	Design and optimization of novel imidazopyridine derivatives led to the identification of a potent and selective PLK inhibitor 36. A novel class of imidazopyridine derivatives was designed as PLK1 inhibitors. Extensive SAR studies supported by molecular modeling afforded a highly potent and selective compound 36. Compound 36 demonstrated good antitumor efficacy in xenograft nude rat model.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.06.084