1380195-33-4Relevant academic research and scientific papers
Solid-phase synthesis of libraries of ethynylated aminosteroid derivatives as potential antileukemic agents
Talbot, Amélie,Maltais, René,Kenmogne, Lucie Carolle,Roy, Jenny,Poirier, Donald
, p. 55 - 64 (2016)
Steroids possessing an ethynyl group at position 17α (tertiary alcohols) are well known to be more stable than their non-ethynyl analogs (secondary alcohols). To facilitate the development of new drugs with better metabolic stability, we developed a new d
New diethylsilylacetylenic linker for parallel solid-phase synthesis of libraries of hydroxy acetylenic steroid derivatives with improved metabolic stability
Talbot, Amelie,Maltais, Rene,Poirier, Donald
scheme or table, p. 347 - 351 (2012/08/08)
Acetylenic tertiary alcohols are well-known to be compounds that are biologically more stable than their corresponding secondary alcohols. The linkage of an acetylenic compound to a polymer support and further introduction of molecular diversity was found to be an interesting way to generate libraries of hydroxy acetylenic derivatives and thus potentially improve their biological properties. For the first time, we describe the loading of an ethynyl steroid to a polystyrene-diethylsilane resin and its uses for the solid-phase synthesis of a model library of 21 steroid derivatives. Two levels of molecular diversity were introduced by successive addition of amino acids and carboxylic acids, and hydroxy acetylenic steroids were then released by an acidic treatment in high yield and purity without further purification step.
