Design of granulatimide and isogranulatimide analogues as potential Chk1 inhibitors: Study of amino-platforms for their synthesis

The two marine alkaloids granulatimide and isogranulatimide have been shown to inhibit the checkpoint kinase 1 (Chk1), a promising target for cancer treatment. A molecular docking study allowing the design of new potential Chk1 inhibitors based on the natural products skeleton and the synthetic work...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2014-09, Vol.22 (17), p.4961-4967
Hauptverfasser:	Lavrard, Hubert, Rodriguez, Frédéric, Delfourne, Evelyne
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkaloids - chemical synthesis Alkaloids - chemistry Alkaloids - pharmacology Checkpoint Kinase 1 Chemical Sciences Chk1 inhibitors Dose-Response Relationship, Drug Drug Design Granulatimide Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - pharmacology Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Isogranulatimide Marine alkaloid Models, Molecular Molecular Structure Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein Kinases - metabolism Structure-Activity Relationship
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Zusammenfassung:	The two marine alkaloids granulatimide and isogranulatimide have been shown to inhibit the checkpoint kinase 1 (Chk1), a promising target for cancer treatment. A molecular docking study allowing the design of new potential Chk1 inhibitors based on the natural products skeleton and the synthetic work to an amino-target platform to prepare them are described.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2014.06.028