The combination of quinazoline and chalcone moieties leads to novel potent heterodimeric modulators of breast cancer resistance protein (BCRP/ABCG2)
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- 作者：Stefanie Kraege1 ; Katja Stefan1 ; Kapil Juvale ; Thomas Ross ; Thomas Willmes ; Michael Wiese ; mwiese@uni-bonn.de" class="auth_mail" title="E-mail the corresponding author
- 关键词：ABC transporter ; ABCG2 ; Multidrug resistance ; Chalcones ; Quinazolines ; Quinazoline-chalcones ; Pheophorbide A assay ; ATPase
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：19 July 2016
- 年：2016
- 卷：117
- 期：Complete
- 页码：212-229
- 全文大小：2673 K
文摘
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Combination of quinazoline and chalcone scaffolds to heterodimeric inhibitors.
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Quinazoline-chalcones are potent inhibitors of ABCG2.
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Most potent compound was found to be selective, non-toxic and able to reverse MDR.
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Stimulate ATPase activity without being transported.
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Three compounds show dual inhibitory behavior.