Synthesis of Novel Rexinoids for Use in Preclinical Trials of Cancer Models

Rexinoids such as Bexarotene have been developed as effective treatments of different diseases including lymphoma, breast cancer, lung cancer, Alzheimer’s disease, and diabetes. This is due to the widespread nature of the retinoid X receptor, which is the target of these drugs, throughout the body. However, Bexarotene is not infallible and has many negative side effects which limit the use of the drug to only a short period of time. This may be fine for chemotherapy, but rexinoids have been proposed to also be effective at preventing cancer as well. This is not currently possible with the side effects seen with approved rexinoids. Due to this, six novel rexinoids were created in hopes of reducing the side effect profile of rexinoids. The idea of dual agonism was also explored with two of the compounds created as well. All six of these compounds, after creation and purification, were sent off for in vitro and in vivo testing to confirm side effect profile and efficacy.