Structure-activity relationship studies on vitamin D lactam derivatives as vitamin D receptor antagonist.
Structure-activity relationship studies on 1alpha,25-dihydroxyvitamin D(3)-26,23-lactams (DLAMs), antagonists of vitamin D, were conducted, focusing on the substituents of the phenyl group. One of the derivatives (23S,25S)-DLAM-1P-3,5(OEt)(2), showed potent antagonistic activity with an IC(50) of 90nM.
Cho
Kaori
K
Department of Biotechnology and Life Science, Faculty of Technology, Tokyo University of Agriculture and Technology, 2-24-16, Naka-cho, Koganei, Tokyo 184-8588, Japan.
Uneuchi
Fumito
F
Kato-Nakamura
Yuko
Y
Namekawa
Jun-ichi
J
Ishizuka
Seiichi
S
Takenouchi
Kazuya
K
Nagasawa
Kazuo
K
D002117:Calcitriol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D007769:Lactams / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D015394:Molecular Structure; D018167:Receptors, Calcitriol / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014807:Vitamin D / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology
C510297:DLAM-1P compound; D007769:Lactams; D018167:Receptors, Calcitriol; D014807:Vitamin D; D002117:Calcitriol