A-ring hydroxymethyl 19-nor analogs of the natural hormone 1α,25-dihydroxyvitamin D_3: synthesis and preliminary biological evaluation

摘要

A series 5-8 of 1- and 3-CH_2OH 19-nor analogs of the hormone calcitriol (1) has been prepared. Surprisingly, 19-nor 1α-CH_2OH analog 5a is more antiproliferative at 100 nM concentration than the corresponding regioisomeric analog 6a with the natural 1α-OH group, and 1α-CH_2OH hybrid analog 7a is similar in antiproliferative potency to calcitriol (1) even at low nanomolar concentrations.