Synthesis and biological evaluation of phosphonate analogues of 1alpha,25-dihydroxyvitamin D3.
A new series of phosphonate side chain analogues of 1alpha,25-dihydroxyvitamin D3 (1) have been synthesized. Antiproliferative activities of theses analogues (8a,b and 9a,b) using human keratinocyte cell shows that analogues which have natural A-ring show higher activity than unnatural A-ring series and almost equally active to 1alpha,25-Dihydroxyvitamin D3 (1) at 1 microM level.
Han
G
G
Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA. gyoonhee.han.gh@bayer.co.jp
D002117:Calcitriol / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology; D002120:Calcium Channel Agonists / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D015603:Keratinocytes / Q000187:drug effects / Q000502:physiology; D063065:Organophosphonates / Q000737:chemistry* / Q000494:pharmacology
D002120:Calcium Channel Agonists; D063065:Organophosphonates; D002117:Calcitriol