An improved route to 19-substituted geldanamycins as novel Hsp90 inhibitors--potential therapeutics in cancer and neurodegeneration

19-Substituted geldanamycin derivatives are efficient Hsp90 inhibitors, without the toxicity associated with the other benzoquinone ansamycins, thus giving them potential for use as molecular therapeutics in cancer and neurodegeneration. Here a new method of synthesising these important compounds is...

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Veröffentlicht in:	Chemical communications (Cambridge, England) England), 2013-01, Vol.49 (76), p.8441
Hauptverfasser:	Kitson, Russell R A, Moody, Christopher J
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Benzoquinones - chemical synthesis Benzoquinones - chemistry Benzoquinones - pharmacology Crystallography, X-Ray Dose-Response Relationship, Drug HSP90 Heat-Shock Proteins - antagonists & inhibitors Humans Lactams, Macrocyclic - chemical synthesis Lactams, Macrocyclic - chemistry Lactams, Macrocyclic - pharmacology Models, Molecular Molecular Conformation Neoplasms - drug therapy Nerve Degeneration - drug therapy Neuroprotective Agents - chemical synthesis Neuroprotective Agents - chemistry Neuroprotective Agents - pharmacology Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	19-Substituted geldanamycin derivatives are efficient Hsp90 inhibitors, without the toxicity associated with the other benzoquinone ansamycins, thus giving them potential for use as molecular therapeutics in cancer and neurodegeneration. Here a new method of synthesising these important compounds is reported, eliminating the need for toxic metals and metalloids.
ISSN:	1359-7345 1364-548X
DOI:	10.1039/c3cc43457e