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

Kelly Chibale; Iwao Ojima; Hayley Haupt; Xugong Geng; Paula Pera; Ralph J. Bernacki

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

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

Kelly Chibale
, Iwao Ojima
, Hayley Haupt
, Xugong Geng
, Paula Pera
, Ralph J. Bernacki

Chemistry

University of Cape Town
Stony Brook University
Roswell Park Cancer Institute

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

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.

Original language	English
Pages (from-to)	2457-2460
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	18
DOIs	https://doi.org/10.1016/S0960-894X(01)00462-0
State	Published - Sep 17 2001

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title = "Modulation of human mammary cell sensitivity to paclitaxel by new quinoline sulfonamides",

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.",

author = "Kelly Chibale and Iwao Ojima and Hayley Haupt and Xugong Geng and Paula Pera and Bernacki, \{Ralph J.\}",

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T1 - Modulation of human mammary cell sensitivity to paclitaxel by new quinoline sulfonamides

AU - Chibale, Kelly

AU - Ojima, Iwao

AU - Haupt, Hayley

AU - Geng, Xugong

AU - Pera, Paula

AU - Bernacki, Ralph J.

PY - 2001/9/17

Y1 - 2001/9/17

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/0035903869

U2 - 10.1016/S0960-894X(01)00462-0

DO - 10.1016/S0960-894X(01)00462-0

M3 - Article

C2 - 11549446

AN - SCOPUS:0035903869

SN - 0960-894X

VL - 11

SP - 2457

EP - 2460

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 18

ER -

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

Abstract

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