Document Detail


Design, Synthesis and Multidrug Resistance Reversal Activity Evaluation of 8-Oxocoptisine Derivatives.
MedLine Citation:
PMID:  22548337     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Fifteen derivatives of 8-oxocoptisine were prepared based on that 8-oxocoptisine showed potent reversing effect against human cancer cells charactering multidrug resistance (MDR). The derivatives were evaluated for their growth inhibition and effects on reversing P-gp-mediated MDR against MCF-7/AMD cells. 12, 13-dinitro-8-oxocoptisine (6c), the most potential candidate with weak growth inhibition, significantly increased the sensitivity of adriamycin (ADM) against MCF-7/ADM cells by 213-fold at 10μM that was compared to the reference compound verapamil. The preliminary structure-activity relationships (SARs) of these derivatives were discussed on the basis of the in vitro MDR reversal activities.
Authors:
Jian Bo Wu; Fan Lei; Xiang Juan Cui; Yun He; Li Hai; Juan Zhang; Yong Wu
Related Documents :
25350317 - Combining a bcl2 inhibitor with the retinoid derivative fenretinide targets melanoma ce...
22853427 - Sequence-dependent synergistic inhibition of human glioma cell lines by combined temozo...
21166897 - Yeev is an escherichia coli toxin that inhibits cell division by targeting the cytoskel...
19011687 - Quantification of cell edge velocities and traction forces reveals distinct motility mo...
23007077 - The impact of potential islet precursor cells on islet autotransplantation outcomes.
8581987 - Artificial cell-spreading of permeabilized bhk cells on fibronectin-coated substratum.
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-4-27
Journal Detail:
Title:  Medicinal chemistry (Shariqah (United Arab Emirates))     Volume:  -     ISSN:  1875-6638     ISO Abbreviation:  -     Publication Date:  2012 Apr 
Date Detail:
Created Date:  2012-5-2     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101240303     Medline TA:  Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
West China School of Pharmacy, Sichuan University, No.17 Section 3, South Renmin Road Chengdu, Sichuan 610041 China. wyong@scu.edu.cn.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:

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


Previous Document:  In vitro Antibacterial and Antifungal Activity of Salicylanilide Pyrazine-2-Carboxylates.
Next Document:  Design, synthesis and antiproliferative activity of 2-acetamidothiazole-5-carboxamide derivatives.