Document Detail


Modulation of human mammary cell sensitivity to paclitaxel by new quinoline sulfonamides.
MedLine Citation:
PMID:  11549446     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Sulfonamide derivatives of chloroquine and primaquine were synthesised and evaluated against both paclitaxel-sensitive and paclitaxel-resistant mammarian cancer cell lines. All derivatives exhibited at least 96% MDR reversal activity when co-administered with paclitaxel at 5 microM. The best compound, a chloroquine derivative, exhibited 99% MDR reversal activity when co-administered with paclitaxel at 1 microM. Molecular modelling studies reveal that these derivatives share a common pharmacophore with taxane MDR reversal agents.
Authors:
K Chibale; I Ojima; H Haupt; X Geng; P Pera; R J Bernacki
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  11     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2001 Sep 
Date Detail:
Created Date:  2001-09-10     Completed Date:  2002-03-12     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  2457-60     Citation Subset:  IM    
Affiliation:
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa. chibale@science.uct.ac.za
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MeSH Terms
Descriptor/Qualifier:
Antimalarials / chemistry,  pharmacology
Antineoplastic Agents / chemistry*,  pharmacology*
Antineoplastic Agents, Phytogenic / pharmacology
Breast Neoplasms / drug therapy*
Drug Design
Drug Resistance, Multiple
Drug Resistance, Neoplasm
Drug Screening Assays, Antitumor
Humans
Inhibitory Concentration 50
Models, Molecular
Paclitaxel / pharmacology*
Quinolines / chemistry
Structure-Activity Relationship
Sulfonamides / chemistry,  pharmacology
Tumor Cells, Cultured
Grant Support
ID/Acronym/Agency:
CA16056/CA/NCI NIH HHS; CA73872/CA/NCI NIH HHS; GM42798/GM/NIGMS NIH HHS
Chemical
Reg. No./Substance:
0/Antimalarials; 0/Antineoplastic Agents; 0/Antineoplastic Agents, Phytogenic; 0/Quinolines; 0/Sulfonamides; 33069-62-4/Paclitaxel; 91-22-5/quinoline

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


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