Document Detail

Papyriferic acid derivatives as reversal agents of multidrug resistance in cancer cells.
MedLine Citation:
PMID:  20363142     Owner:  NLM     Status:  MEDLINE    
Forty-one derivatives of papyriferic acid were prepared based on our previous finding that methyl papyriferate (3) showed potent reversing effect on cytotoxicity of colchicine against multidrug resistance (MDR) human cancer cells (KB-C2), and evaluated for their cytotoxicity and effect on reversing P-gp-mediated MDR against KB-C2 cells. 3-O-(Morpholino-beta-oxopropanoyl)-12beta-acetoxy-3alpha,25-dihydroxy-(20S,24R)-epoxydammarane (37) significantly increased the sensitivity of colchicine against KB-C2 cells by 185-fold at 5microg/mL (7.4microM), and the cytotoxicity of colchicine was recovered to nearly that of sensitive (KB) cells. The other several new amide derivatives also exhibited potent reversal activity comparable to or more potent than methyl papyriferate and verapamil.
Juan Xiong; Masatoshi Taniguchi; Yoshiki Kashiwada; Michiko Sekiya; Takashi Yamagishi; Yoshihisa Takaishi
Publication Detail:
Type:  Journal Article     Date:  2010-03-06
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  18     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2010 Apr 
Date Detail:
Created Date:  2010-04-12     Completed Date:  2010-07-16     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  2964-75     Citation Subset:  IM    
Copyright Information:
Copyright 2010 Elsevier Ltd. All rights reserved.
Graduate School of Pharmaceutical Sciences, University of Tokushima, Tokushima 770-8505, Japan.
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MeSH Terms
Antineoplastic Agents / chemical synthesis,  chemistry*,  toxicity
Cell Line, Tumor
Drug Resistance, Multiple
Drug Resistance, Neoplasm
Malonates / chemical synthesis,  chemistry*,  toxicity
Morpholines / chemical synthesis,  chemistry*,  pharmacology
P-Glycoprotein / metabolism
Triterpenes / chemical synthesis,  chemistry*,  pharmacology,  toxicity
Reg. No./Substance:
0/3-O-(morpholino-beta-oxopropanoyl)-12beta-acetoxy-3alpha,25-dihydroxy-(20S,24R)-epoxydammarane; 0/Antineoplastic Agents; 0/Malonates; 0/Morpholines; 0/P-Glycoprotein; 0/Triterpenes; 0/papyriferic acid

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