Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Benzoquinones / chemical synthesis
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Benzoquinones / chemistry
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Benzoquinones / pharmacology*
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Crystallography, X-Ray
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Dose-Response Relationship, Drug
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HSP90 Heat-Shock Proteins / antagonists & inhibitors*
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Humans
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Lactams, Macrocyclic / chemical synthesis
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Lactams, Macrocyclic / chemistry
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Lactams, Macrocyclic / pharmacology*
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Models, Molecular
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Molecular Conformation
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Neoplasms / drug therapy*
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Nerve Degeneration / drug therapy*
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Neuroprotective Agents / chemical synthesis
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Neuroprotective Agents / chemistry
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Neuroprotective Agents / pharmacology*
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Benzoquinones
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HSP90 Heat-Shock Proteins
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Lactams, Macrocyclic
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Neuroprotective Agents
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geldanamycin