Document Detail

Sterols as anticancer agents: synthesis of ring-B oxygenated steroids, cytotoxic profile, and comprehensive SAR analysis.
MedLine Citation:
PMID:  20931970     Owner:  NLM     Status:  MEDLINE    
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.
João F S Carvalho; M Manuel Cruz Silva; João N Moreira; Sérgio Simões; M Luisa Sá e Melo
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  53     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2010 Nov 
Date Detail:
Created Date:  2010-11-04     Completed Date:  2010-12-28     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  7632-8     Citation Subset:  IM    
Center for Pharmaceutical Studies, University of Coimbra, Portugal.
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MeSH Terms
Antineoplastic Agents / chemical synthesis*,  chemistry,  pharmacology
Antineoplastic Combined Chemotherapy Protocols / pharmacology
Cell Line
Cell Line, Tumor
Cell Proliferation / drug effects
Cisplatin / administration & dosage
Doxorubicin / administration & dosage
Drug Screening Assays, Antitumor
Drug Synergism
Sterols / chemical synthesis*,  chemistry,  pharmacology
Structure-Activity Relationship
Reg. No./Substance:
0/Antineoplastic Agents; 0/Sterols; 15663-27-1/Cisplatin; 23214-92-8/Doxorubicin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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