Document Detail

Selective cytotoxic activities of two novel synthetic drugs on human breast carcinoma MCF-7 cells.
MedLine Citation:
PMID:  19661306     Owner:  NLM     Status:  MEDLINE    
BACKGROUND: Breast cancer is the second leading cause of cancer deaths in US women. We evaluated two novel compounds, piperidinyl-diethylstilbestrol (DES) and pyrrolidinyl-diethylstilbestrol (DES) for cytotoxicity against brine shrimp larvae, MCF-7 and rat normal liver cells.
MATERIALS AND METHODS: In vivo cytotoxicity was evaluated against shrimp larvae for 24 h, while in vitro cell toxicity was evaluated by dye binding crystal-violet method after 48 h. The role of these compounds on different phases of the cell cycle was assessed by flow cytometry.
RESULTS: In shrimp assay, piperidinyl-DES and pyrrolidinyl-DES were potent with 50% effective dose (ED(50)) values of 7.9+/-0.38 and 15.6+/-1.3 microM, respectively. In MCF-7 and normal liver cells, the 50% lethal concentration (LC(50)) values were 19.7+/-0.95, 17.6+/-0.4 microM and 35.1 and >50 microM, respectively. Cell cycle analyses indicated that MCF-7 cells were arrested at the G(0)/G(1) stage with these compounds.
CONCLUSION: The results indicate that pyrrolidinyl-DES possesses highly selective, potent anticancer activity.
Ramesh B Badisa; Selina F Darling-Reed; Patrick Joseph; John S Cooperwood; Lekan M Latinwo; Carl B Goodman
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Anticancer research     Volume:  29     ISSN:  1791-7530     ISO Abbreviation:  Anticancer Res.     Publication Date:  2009 Aug 
Date Detail:
Created Date:  2009-08-07     Completed Date:  2009-09-30     Revised Date:  2013-06-02    
Medline Journal Info:
Nlm Unique ID:  8102988     Medline TA:  Anticancer Res     Country:  Greece    
Other Details:
Languages:  eng     Pagination:  2993-6     Citation Subset:  IM    
College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL-32307, USA.
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MeSH Terms
Adenocarcinoma / drug therapy,  pathology*
Antineoplastic Agents / chemical synthesis,  pharmacology*
Apoptosis / drug effects*
Artemia / drug effects*
Biological Assay / methods
Breast Neoplasms / drug therapy,  pathology*
Cell Cycle / drug effects
Flow Cytometry
Larva / drug effects
Liver / drug effects
Piperidines / chemical synthesis*,  pharmacology*
Pyrrolidines / chemical synthesis*,  pharmacology*
Stilbenes / chemical synthesis*,  pharmacology*
Grant Support
G12 RR003020/RR/NCRR NIH HHS; G12 RR003020-255370/RR/NCRR NIH HHS; G12 RR003020-255372/RR/NCRR NIH HHS; G12RR03020/RR/NCRR NIH HHS; GM08111/GM/NIGMS NIH HHS; SD34HP04018//PHS HHS
Reg. No./Substance:
0/Antineoplastic Agents; 0/Piperidines; 0/Pyrrolidines; 0/Stilbenes

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