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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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-08, Vol.19 (16), p.4673-4678
Main Authors: 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: Article
Language:English
Subjects:
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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Summary: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