Tariquidar-Related Chalcones and Ketones as ABCG2 Modulators.

ABSTRACT: ABC transporters, including ABCG2, play a vital role in defending the human body against the vast range of xenobiotics. Even though this is beneficial for human health, these protein transporters have been implicated in the emerging resistance of cancer cells to a variety of structurally and functionally diverse anticancer drugs. In order to investigate their role in resistance, potent and selective ABCG2 modulators have been described in the literature. A leading class of modulators are the tariquidar analogues; however, their susceptibility to hydrolysis limits their applicable use. To overcome this, we synthesized a novel series of chalcone- and ketone-based compounds inspired by reported tariquidar analogues. Compounds were characterized and evaluated for their ABCG2 modulatory activit

SUBMITTER: Pena-Solorzano D 

PROVIDER: S-EPMC6088357 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature