Literature summary for 7.6.2.2 extracted from

Palmeira, A.; Vasconcelos, M.H.; Paiva, A.; Fernandes, M.X.; Pinto, M.; Sousa, E.
Dual inhibitors of P-glycoprotein and tumor cell growth: (re)discovering thioxanthones (2012), Biochem. Pharmacol., 83, 57-68.

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Inhibitors

Inhibitors	Comment	Organism	Structure
1-(4-acetylpiperazin-1-yl)-4-propoxy-9H-thioxanthen-9-one	uncompetitive, approximately 1.5fold more potent than verapamil in decreasing the doxorubicin GI50 on K-562 Dox cell line	Homo sapiens
1-[[2-(4-nitrophenyl)ethyl]amino]-4-propoxy-9H-thioxanthen-9-one	uncompetitive, approximately 1.5fold more potent than verapamil in decreasing the doxorubicin GI50 on K-562 Dox cell line	Homo sapiens
[2-(1H-benzimidazol-2-yl)ethanamine]-4-propoxy-9H-thioxanthen-9-one	uncompetitive, causes an accumulation rate of rhodamine-123 similar to that caused by verapamil in the K-562 Dox resistant cell line, and a decrease in ATP consumption by P-gp. At 10 mM, 12.5fold decrease in the GI50 value of doxorubicin in the K-562 Dox resistant cell line, being 2fold more potent than verapamil	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
K-562 cell	-	Homo sapiens	-

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Release 2023.1 (January 2023)