Abstract
The cytotoxicity of oxysterols was systematically studied in tumor and normal cells. Synthetic strategies to prepare this library included oxidations at ring B and a new method to yield 6β-hemiphthalates directly from Δ(5)-steroids. Most oxysterols were cytotoxic and showed selectivity toward cancer cells, LAMA-84 cells (leukemia) being particularly sensitive to 4, 8, 22, and 27 (IC(50) < 5.6 μM). The structural requirements to induce selective toxicity are discussed to shed light on the development of new anticancer drugs.
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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Antineoplastic Combined Chemotherapy Protocols / pharmacology
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Cell Line
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cisplatin / administration & dosage
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Doxorubicin / administration & dosage
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Drug Screening Assays, Antitumor
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Drug Synergism
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Humans
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Sterols / chemical synthesis*
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Sterols / chemistry
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Sterols / pharmacology
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Sterols
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Doxorubicin
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Cisplatin