51238-15-4Relevant academic research and scientific papers
Synthesis of [D4]- and [D7]-4β- hydroxycholesterols for use in a novel drug-drug interaction assay
Turley, Wesley A.,Burrell, Richard C.,Bonacorsi Jr., Samuel J.,Goodenough, Angela K.,Onorato, Joelle M.
scheme or table, p. 61 - 65 (2012/06/30)
Cytochrome P450 3A (CYP3A) enzymes are involved in the metabolism of over half of today's prescription drugs. As a result, drugs metabolized by CYP3A have a risk of drug-drug interactions (DDIs). Recent studies have shown the potential to use 4β-hydroxych
Synthesis and evaluation of new 6-hydroximinosteroid analogs as cytotoxic agents
Poza, Javier,Rega, Miriam,Paz, Vanessa,Alonso, Beatriz,Rodriguez, Jaime,Salvador, Nelida,Fernandez, Antonio,Jimenez, Carlos
, p. 4722 - 4740 (2008/03/13)
Taking into account the structural requirements for cytotoxicity, several new hydroximinosteroid derivatives have been prepared and evaluated for their cytotoxic activity against A-549, H116, PSN1, and T98G cultured tumor cell lines in order to obtain further information on the potential pharmacophoric core of this type of compound. The influence of the oxygenated position in the A ring, the presence of an additional oxygenated position at C-7 and C-16, and a fluorinated position at C-5 were considered in order to study the structure-activity relationships. The results reveal the importance of oxygenated positions in the A ring (e.g., 4,5-epoxide showed an IC50 value against HCT-116 under micromolar level) for an increase in cytotoxic activity in this type of compound. Furthermore, they showed an important selectivity toward colon tumor line (HCT-116).
