A three-step synthesis from rebeccamycin of an efficient checkpoint kinase 1 inhibitor
Fabrice Anizon1, Roy M Golsteyn, Stéphane Léonce
1Université Blaise Pascal, Synthèse et Etude de Systèmes à Intérêt Biologique, UMR 6504 du CNRS, 63177 Aubière, France.
European Journal of Medicinal Chemistry
|July 8, 2008
Abstract:
Rebeccamycin derivative 1 bearing a sugar moiety linked to both indole nitrogens and an amino substituent on the carbohydrate unit was synthesized in three steps from the bacterial metabolite. This compound was found to be a highly potent checkpoint kinase 1 inhibitor with an IC(50) value of 2.8nM.
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