Synthesis and structure–activity evaluation of isatin-β-thiosemicarbazones with improved selective activity toward multidrug-resistant cells expressing P-glycoprotein

MD Hall, KR Brimacombe, MS Varonka…

Index: Hall, Matthew D.; Brimacombe, Kyle R.; Varonka, Matthew S.; Pluchino, Kristen M.; Monda, Julie K.; Li, Jiayang; Walsh, Martin J.; Boxer, Matthew B.; Warren, Timothy H.; Fales, Henry M.; Gottesman, Michael M. Journal of Medicinal Chemistry, 2011 , vol. 54, # 16 p. 5878 - 5889

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Citation Number: 59

Abstract

Cancer multidrug resistance (MDR) mediated by ATP-binding cassette (ABC) transporters presents a significant unresolved clinical challenge. One strategy to resolve MDR is to develop compounds that selectively kill cells overexpressing the efflux transporter P- glycoprotein (MDR1, P-gp, ABCB1). We have previously reported structure–activity studies based around the lead compound NSC73306 (1, 1-isatin-4-(4′-methoxyphenyl)-3- ...