Novel halogenated sulfonamides inhibit the growth of multidrug resistant MCF-7/ADR cancer cells.
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 beta-tubulin. Consistent with this mechanism of action, the cytotoxicities of these compounds appear to correlate with their ability to undergo nucleophilic aromatic substitution.
Tularik Inc., South San Francisco, CA 94080, USA.
J C
JC
Medina
D
D
Roche
B
B
Shan
R M
RM
Learned
W P
WP
Frankmoelle
D L
DL
Clark
T
T
Rosen
J C
JC
Jaen
D018432:Drug Resistance, Multiple; D006131:Growth Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006219:Halogens / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D006131:Growth Inhibitors; D006219:Halogens; D013449:Sulfonamides