Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 95, Issue -, Pages 35-40Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.03.020
Keywords
Spirooxindoles; CFI-400945; Anticancer drug; Kinase selectivity
Categories
Funding
- Natural Science Foundation of China [21372206]
- Development Foundation of Priority, Ministry of Education [20134101130001]
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The identification of novel anticancer agents with high efficacy and low toxicity has always been an intriguing topic in medicinal chemistry. The unique structural features of spirooxindoles together with diverse biological activities have made them promising structures in new drug discovery. Among spirooxindoles, CFI-400945 holds its promise as the first potent PLK4 inhibitor, the fumarate of CFI-400945 has entered phase I clinical trials for the treatment of solid tumors. However, questions remain as to whether PLK4 is the only relevant therapeutic target for CFI-400945. To highlight this significant progress of CFI-400945 in last two years, this review centers on the identification from a focused kinase library, structural optimizations and strategies involved, structure-activity relationships, modes of action, target validation, chemical synthesis and, more importantly, the kinase selectivity between PLK4 and other targets. (C) 2015 Elsevier Masson SAS. All rights reserved.
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