Authors: Steinmeyer, Andreas; Kirsch, Gerald; Neef, Gunter; Schwarz, Katica

Source: Current Pharmaceutical Design, Volume 6, Number 7, May 2000 , pp. 767-789(23)

Publisher: Bentham Science Publishers

Abstract:

The introduction of oxygen atoms into different positions of the vitamin D side chain is described. By combining the arising 23-oxa and 25-oxa elements with other structural modifications (19-nor, iso-19-nor, 20-methyl, 20-ene, 20,21-cyclo) calcitriol analogs with remarkable levels of dissociation between beneficial acitivities on cell growth regulation and undesired hypercalcemia were identified. Structure-activity relations are elaborated in a very systematic outline of the Schering drug finding program in this particular class of vitamin D compounds.

Keywords: Antiproliferative Activities; 23 Oxa Calcitriols; 19 Nor 23 oxa Calcitriols; Iso 19 nor 23 oxa Calcitriols; 20 Methyl 23 oxa calcitriols; 20 Ene 23 oxa Calcitriol; 20 Ene 19 nor 23 oxa Calcitriols; 20 21 Cyclo 23 oxa calcitriols; 25 oxa Calcitriols; Relative binding affinity; Vitamin D receptor; 1 4 Diazabicyclo 2 2 2 octane; Diisobutylaluminum hydride; Vitamin D binding prtien; Human leukemia cell line; Lithium diisopropylamide; Relative binding affinity; Vitamin D receptor

Document Type: Research article

Affiliations: 1: Schering AG, Institute of Medicinal Chemistry, D-13342 Berlin, Germany

Publication date: 2000-05-01

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