Synthesis and evaluation of new 6-hydroximinosteroid analogs as cytotoxic agents.


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).


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@article{Poza2007SynthesisAE, title={Synthesis and evaluation of new 6-hydroximinosteroid analogs as cytotoxic agents.}, author={Javier Jes{\'u}s Poza and Miriam Rega and Vanessa Paz and Beatriz Dur{\'a}n Alonso and Jaime Rodr{\'i}guez and N{\'e}lida Salvador and Antonio Fern{\'a}ndez and Carlos Jim{\'e}nez}, journal={Bioorganic & medicinal chemistry}, year={2007}, volume={15 14}, pages={4722-40} }