Synthesis, Resolution, and Biological Evaluation of Atropisomeric (aR)- and (aS)‑16-Methyllamellarins N: Unique Effects of the Axial Chirality on the Selectivity of Protein Kinases Inhibition

The total synthesis of the optically active (aR)- and (aS)-16-methyllamellarins N (3a and 3b) was achieved via resolution on HPLC chiral stationary phase. The kinase inhibitory activities of both enantiomers were evaluated on eight protein kinases relevant to cancer and neurodegenerative diseases (C...

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Veröffentlicht in:	Journal of medicinal chemistry 2013-09, Vol.56 (18), p.7289-7301
Hauptverfasser:	Yoshida, Kenyu, Itoyama, Ryosuke, Yamahira, Masashi, Tanaka, Junji, Loaëc, Nadège, Lozach, Olivier, Durieu, Emilie, Fukuda, Tsutomu, Ishibashi, Fumito, Meijer, Laurent, Iwao, Masatomo
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - metabolism Antineoplastic Agents - pharmacology Cell Line, Tumor Chemistry Techniques, Synthetic DNA Topoisomerases, Type I - chemistry DNA Topoisomerases, Type I - metabolism Humans Molecular Docking Simulation Polycyclic Compounds - chemical synthesis Polycyclic Compounds - chemistry Polycyclic Compounds - metabolism Polycyclic Compounds - pharmacology Protein Conformation Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - metabolism Protein Kinase Inhibitors - pharmacology Protein Kinases - chemistry Protein Kinases - metabolism Stereoisomerism Structure-Activity Relationship Substrate Specificity Topoisomerase I Inhibitors - chemical synthesis Topoisomerase I Inhibitors - chemistry Topoisomerase I Inhibitors - metabolism Topoisomerase I Inhibitors - pharmacology
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