Strategies for improving the solubility and metabolic stability of griseofulvin analogues

We report two types of modifications to the natural product griseofulvin as strategies to improve solubility and metabolic stability: the conversion of aryl methyl ethers into aryl difluoromethyl ethers at metabolic hotspots and the conversion of the C-ring ketone into polar oximes. The syntheses of...

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Veröffentlicht in:	European journal of medicinal chemistry 2016-06, Vol.116, p.210-215
Hauptverfasser:	Petersen, A.B., Konotop, G., Hanafiah, N.H.M., Hammershøj, P., Raab, M.S., Krämer, A., Clausen, M.H.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anticancer Antifungal Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - metabolism Antineoplastic Agents - pharmacology Drug Stability Griseofulvin - chemical synthesis Griseofulvin - chemistry Griseofulvin - metabolism Griseofulvin - pharmacology Griseofulvin analogues HeLa Cells Humans Male Metabolic stability Mice Microsomes - metabolism Oxidation-Reduction Rats Solubility Structure-Activity Relationship Synthesis Thermodynamics
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