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Project Description:

The objective of this project is to synthesize and discover novel ethacrynic acid (EA) derivatives lacking the α,β-unsaturated carbonyl unit, that possess a high potency against cancer cells, especially against invasive cancer cells, to prevent the metastatic process. Prevention of metastases formation is an essential aspect of cancer research because the metastatic spread of primary tumors to distant sites constitutes the most lethal aspect of cancer. Despite extensive research, the exact mechanisms of local invasion and the formation of metastases are still not entirely understood. The development and evaluation of biologically active compounds will give additional insight into this process and would therefore allow the development of new therapeutics that can effectively slow down or even prevent the metastatic process and consequently improve the treatment of success of cancer patients. Testing these derivatives against several human cancer cell lines for their anti-cancer properties will give us a better idea of the structure-activity relationship of these compounds. This knowledge will aid in the process of developing new anti-cancer drugs. Cancer is one of the major causes of death in the U.S. and accounts for 22% of all annual deaths. The mortality of cancer patients is largely caused by tumor invasiveness, leading to local or metastatic tissue destruction. The discovery of new potential anti-cancer drugs and especially anti-metastatic agents will lead to significant progress in the treatment of cancer. Our extensive library of various derivatives of EA will improve the knowledge about the structural influence on the anti-tumor activity significantly. This knowledge will help promote the development of novel, highly active, less toxic, and well-tolerated drugs for patients. The work focuses on I.) Synthesis of EA derivatives lacking the α,β-unsaturated carbonyl unit. II.) Screening of these compounds for their cytotoxic, anti-proliferative, anti-migratory, anti-invasive, and anti-adhesive properties. III.) According to the obtained results, modification of the active compounds will be carried out in order to obtain even more active analogues.