| Modulation of human mammary cell sensitivity to paclitaxel by new quinoline sulfonamides. | |
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MedLine Citation:
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PMID: 11549446 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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K Chibale; I Ojima; H Haupt; X Geng; P Pera; R J Bernacki |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S. |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 11 ISSN: 0960-894X ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2001 Sep |
Date Detail:
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Created Date: 2001-09-10 Completed Date: 2002-03-12 Revised Date: 2007-11-14 |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 2457-60 Citation Subset: IM |
Affiliation:
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Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa. chibale@science.uct.ac.za |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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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:
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CA16056/CA/NCI NIH HHS; CA73872/CA/NCI NIH HHS; GM42798/GM/NIGMS NIH HHS |
| Chemical | |
Reg. No./Substance:
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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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