Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 7.6.2.2 extracted from

  • Hall, M.D.; Brimacombe, K.R.; Varonka, M.S.; Pluchino, K.M.; Monda, J.K.; Li, J.; Walsh, M.J.; Boxer, M.B.; Warren, T.H.; Fales, H.M.; Gottesman, M.M.
    Synthesis and structure-activity evaluation of isatin-beta-thiosemicarbazones with improved selective activity toward multidrug-resistant cells expressing P-glycoprotein (2011), J. Med. Chem., 54, 5878-5889.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 7.6.2.2

Inhibitors

Inhibitors Comment Organism Structure
1-isatin-4-(40-methoxyphenyl)-3-thiosemicarbazone IC50 against KB-3-1 cells 0.0142 mM, against KB-VI cells 0.0033 mM. Displays MDR1-selectivity against all P-glycoprotein expressing cell lines examined, and cross-resistance is no observed. Selectivity is reversed by inhibitors of P-glycoprotein ATPase activity. Compound also shows selectivity for cells expressing mouse and hamster MDR1 Homo sapiens
1-isatin-4-(40-nitrophenyl)-3-thiosemicarbazone IC50 against KB-3-1 cells 0.0171 mM, against KB-VI cells 0.0021 mM Homo sapiens
1-isatin-4-(40-tert-butyl phenyl)-3-thiosemicarbazone IC50 against KB-3-1 cells 0.0159 mM, against KB-VI cells 0.0148 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
KB-3-1 cell
-
 Homo sapiens
-
KB-V1 cell overexpression of P-glycoprotein Homo sapiens
-