Background: Melanoma is the most lethal type among skin cancers, causing about 75% of all skin cancer deaths. Inhibition of the Mitogen Activated Protein Kinsase Pathway (MAPK) signaling at any level can assist in the treatment of melanoma. Minor modifications of the estrange structure can result in extensive changes in biological activity.
Description: SDSU researchers have designed and synthesized analogs based on the estrone skeleton by employing a computer aided drug design approach followed by the biological evaluation for the synthesized analogs. These analogs have shown potential activity as a drug candidate targeting melanoma. Second generation estrone analogs can be a viable route for obtaining non-ATP competitive inhibitors.
Advantages: The analogs offer a novel and potential scaffolds towards the treatment of melanoma while offering new strategies towards the treatment of melanoma