
Bioorganic and Medicinal Chemistry Letters p. 1843 - 1846 (1999)
Update date:2022-08-02
Topics:
Medina, Julio C.
Roche, Daniel
Shan, Bei
Learned, R. Marc
Frankmoelle, Walter P.
Clark, David L.
Rosen, Terry
Jaen, Juan C.
In this report, we describe the synthesis of halogenated benzenesulfonamide compounds and their ability to inhibit the growth of HeLa, MCF-7 and MCF-7/ADR tumor cells in vitro. The multidrug resistance (MDR) phenotype of certain cells does not affect their sensitivity to these compounds. These agents belong to a family of compounds previously shown to bind irreversibly to cysteine-239 of β-tubulin. Consistent with this mechanism of action, the cytotoxicities of these compounds appear to correlate with their ability to undergo nucleophilic aromatic substitution.
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