Document Detail

Fatty acyl amide derivatives of doxorubicin: Synthesis and in vitro anticancer activities.
MedLine Citation:
PMID:  21420207     Owner:  NLM     Status:  Publisher    
Doxorubicin is extensively used in anticancer therapy. Doxorubicin is highly hydrophilic, has short half-life, and its use is associated with severe side effects at high doses. Fatty acyl amide derivatives of doxorubicin were synthesized with the expectation to improve the lipophilicity and anticancer activity of the drug. The lipophilicity was enhanced with the increase in chain length of fatty acyl moiety. Conjugation of 4'-amino group with fatty acids through an amide bond reduced the anticancer activity in leukemia, breast, ovarian, and colon cancer cell lines, suggesting that the presence of free amino group is required for anticancer activity of doxorubicin. Dodecanoyl-doxorubicin derivative was consistently the most effective among the synthesized derivatives and inhibited the proliferation of colon (HT-29) and ovarian (SK-OV-3) cancer cells by 64% and 58%, respectively, at a concentration of 1 μM after 96 h incubation.
Bhupender S Chhikara; Nicole St Jean; Deendayal Mandal; Anil Kumar; Keykavous Parang
Related Documents :
7127737 - Four methods for determining uric acid compared with a candidate reference method.
2396747 - Continuous flow molecular emission cavity analysis of cephalosporins by alkaline degrad...
17316227 - Examination of the steps leading up to the physical developer process for developing fi...
21821957 - Post-translational isoprenylation of tryptophan.
2403257 - Tetrachloroethene transformation to trichloroethene and cis-1,2-dichloroethene by sulfa...
2072097 - Incorporation of very-long-chain fatty acids into sphingolipids of cultured neural cells.
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-3-3
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  -     ISSN:  1768-3254     ISO Abbreviation:  -     Publication Date:  2011 Mar 
Date Detail:
Created Date:  2011-3-22     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 Elsevier Masson SAS. All rights reserved.
Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, 41 Lower College Road, Kingston, RI 02881, USA.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms

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

Previous Document:  N-Acylaminophenothiazines: Neuroprotective agents displaying multifunctional activities for a potent...
Next Document:  Support for nursing and midwifery students: A special case?