Document Detail


Synthesis, proapoptotic screening, and structure-activity relationships of novel aza-lupane triterpenoids.
MedLine Citation:
PMID:  20719505     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Apoptosis is a highly regulated process by which excessive cells are eliminated in order to maintain normal cell development and tissue homeostasis. Resistance to apoptosis often contributes to failure in cancer prevention and treatment. Apoptotic cell death regulators are considered important targets for discovery and development of new therapeutic agents in oncology research. A class of novel aza-lupane triterpenoids were designed, synthesized, and evaluated for antitumor activity against a panel of cancer cell lines of different histogenic origin and for ability to induce apoptosis. 3,30-Bis(aza) derivatives were identified not only to possess improved cytotoxicity compared to the natural product betulinic acid but also to affect cell death predominantly via apoptosis, whereas the mono(aza) derivatives apparently triggered cell death via different, non-apoptotic pathway(s).
Authors:
Aye Aye Mar; Erika L Szotek; Ali Koohang; William P Flavin; David A Eiznhamer; Michael T Flavin; Ze-Qi Xu
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Publication Detail:
Type:  Journal Article     Date:  2010-08-03
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-08-30     Completed Date:  2010-12-28     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  5389-93     Citation Subset:  IM    
Copyright Information:
Copyright (c) 2010 Elsevier Ltd. All rights reserved.
Affiliation:
Advanced Life Sciences, Inc., 1440 Davey Road, Woodridge, IL 60517, United States.
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MeSH Terms
Descriptor/Qualifier:
Antineoplastic Agents / chemical synthesis,  chemistry*,  pharmacology*
Apoptosis / drug effects*
Cell Line, Tumor
Cytotoxins / chemical synthesis,  chemistry,  pharmacology
Drug Screening Assays, Antitumor
Humans
Neoplasms / drug therapy
Structure-Activity Relationship
Triterpenes / chemical synthesis,  chemistry*,  pharmacology*
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/Cytotoxins; 0/Triterpenes; 464-99-3/lupane; 472-15-1/betulinic acid

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


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