Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors.
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.
Sato
Yoshiyuki
Y
Banyu Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co, Ltd, Tsukuba, Ibaraki 300-2611, Japan.
Onozaki
Yu
Y
Sugimoto
Tetsuya
T
Kurihara
Hideki
H
Kamijo
Kaori
K
Kadowaki
Chie
C
Tsujino
Toshiaki
T
Watanabe
Akiko
A
Otsuki
Sachie
S
Mitsuya
Morihiro
M
Iida
Masato
M
Haze
Kyosuke
K
Machida
Takumitsu
T
Nakatsuru
Yoko
Y
Komatani
Hideya
H
Kotani
Hidehito
H
Iwasawa
Yoshikazu
Y
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018797:Cell Cycle Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D045744:Cell Line, Tumor; D003198:Computer Simulation; D006367:HeLa Cells; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008956:Models, Chemical; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011518:Proto-Oncogene Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D023041:Xenograft Model Antitumor Assays; D000097869:Polo-Like Kinase 1
D000970:Antineoplastic Agents; D018797:Cell Cycle Proteins; D007093:Imidazoles; D047428:Protein Kinase Inhibitors; D017346:Protein Serine-Threonine Kinases; D011518:Proto-Oncogene Proteins; D011725:Pyridines; D000097869:Polo-Like Kinase 1