New 1 alpha,25-dihydroxy vitamin D3 analogues with side chains attached to C-18: synthesis and biological activity.
A new class of analogues of 1 alpha,25-dihydroxy vitamin D3 has been synthesised, in which the side chain (C-23 to C-27) has been removed and where new hydroxylated side chains have been attached to the C-18 methyl group. These analogues show antiproliferative activity in U937 and HaCaT cells comparable to that of 1 alpha,25-dihydroxy vitamin D3. Lack of calcemic activity makes these analogues potentially useful in the treatment of proliferative diseases.
Grue-Sørensen
G
G
Department of Chemical Research, Leo Pharmaceutical Products, Ballerup, Denmark. gunnar.soerensen@leo.dk
Hansen
C M
CM
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002117:Calcitriol / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism / Q000652:urine; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D002645:Chickens; D006801:Humans; D006900:Hydroxylation; D007202:Indicators and Reagents; D015603:Keratinocytes / Q000187:drug effects; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D011201:Poultry Diseases / Q000378:metabolism; D051381:Rats; D018167:Receptors, Calcitriol / Q000187:drug effects / Q000378:metabolism; D012279:Rickets / Q000378:metabolism / Q000662:veterinary; D020298:U937 Cells
D000970:Antineoplastic Agents; D007202:Indicators and Reagents; D018167:Receptors, Calcitriol; D002117:Calcitriol; D002118:Calcium