4-Isoxazolyl-1,4-dihydropyridines exhibit binding at the multidrug-resistance transporter.
The 4-isoxazolyl-dihydropyridines (IDHPs) exhibit inhibition of the multidrug-resistance transporter (MDR-1), and exhibit an SAR distinct from their activity at voltage gated calcium channels (VGCC). Among the four most active IDHPs, three were branched at C-5 of the isoxazole, including the most active analog, 1k.
Department of Chemistry, University of Idaho, Moscow, ID 83844-2343, United States.
Victoria
V
Hulubei
Scott B
SB
Meikrantz
David A
DA
Quincy
Tina
T
Houle
John I
JI
McKenna
Mark E
ME
Rogers
Scott
S
Steiger
N R
NR
Natale
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D018938:Caco-2 Cells; D015220:Calcium Channels / Q000737:chemistry / Q000378:metabolism; D003997:Dicarbethoxydihydrocollidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D004095:Dihydropyridines / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D007555:Isoxazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism*; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D011485:Protein Binding; D013329:Structure-Activity Relationship; D013816:Thermodynamics
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D015220:Calcium Channels; D004095:Dihydropyridines; D007555:Isoxazoles; C578971:diethyl 2,6-dimethyl-4-(5-(1'-m-bromophenylprop-2'-yl)-3-methylisoxazol-4-yl)-1,4-dihydropyridine-3,5-dicarboxylate; D003997:Dicarbethoxydihydrocollidine