ChloroquineV1, Main, Exploration, bibRecord, 002269

Modulation of human mammary cell sensitivity to paclitaxel by new quinoline sulfonamides

Identifieur interne : 002269 ( Main/Exploration ); précédent : 002268; suivant : 002270

Modulation of human mammary cell sensitivity to paclitaxel by new quinoline sulfonamides

Auteurs : Kelly Chibale [Afrique du Sud] ; Iwao Ojima [États-Unis] ; Hayley Haupt [Afrique du Sud] ; Xugong Geng [États-Unis] ; Paula Pera [États-Unis] ; Ralph J. Bernacki [États-Unis]

Source :

Bioorganic & Medicinal Chemistry Letters [ 0960-894X ] ; 2001.

RBID : ISTEX:BC158FC2EAF21BBFB90A1FCB60068D6F224DB5DB

English descriptors

Teeft :
- Acyl moiety, Anticancer, Antimalarial, Benzophenone moiety, Bioorg, Cancer cell lines, Cancer inst, Cell lines, Cell sensitivity, Chem, Chibale, Chloroquine, Common pharmacophore, Conformers, Derivative, Elsevier science, Growth inhibition, Labelling, Labelling taxoid, Lett, Mdrr, Mdrr agents, Modelling, Moiety, Molecular modelling study, Naphthalene group, Paclitaxel, Paclitaxel chemosensitising agents, Pharmacol, Phenyl, Phenyl group, Primaquine, Quinoline, Quinolines, Resultant conformers, Reversal, Reversal activity, Sulfonamide, Taxane mdrr agents, Taxoid, Tras.

Abstract

Abstract: 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 μM. The best compound, a chloroquine derivative, exhibited 99% MDR reversal activity when co-administered with paclitaxel at 1 μM. Molecular modelling studies reveal that these derivatives share a common pharmacophore with taxane MDR reversal agents.

Graphicfx5255

Url:

https://api.istex.fr/ark:/67375/6H6-R7XRVT46-V/fulltext.pdf

DOI: 10.1016/S0960-894X(01)00462-0

Affiliations:

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Le document en format XML

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<front><div type="abstract" xml:lang="en">Abstract: 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 μM. The best compound, a chloroquine derivative, exhibited 99% MDR reversal activity when co-administered with paclitaxel at 1 μM. Molecular modelling studies reveal that these derivatives share a common pharmacophore with taxane MDR reversal agents.</div>
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Modulation of human mammary cell sensitivity to paclitaxel by new quinoline sulfonamides

Modulation of human mammary cell sensitivity to paclitaxel by new quinoline sulfonamides

Source :

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Le document en format XML

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