Novel Focal Adhesion Kinase autophosphorylation inhibitors against pancreatic cancer

DESCRIPTION (provided by applicant): Due to the absence of effective therapies, pancreatic cancer is the fourth leading cause of cancer deaths in both men and women. This study focuses on the development of new small molecule inhibitors targeting Focal Adhesion Kinase against pancreatic cancer. Focal Adhesion Kinase (FAK) has been shown to play an important role in tumor cell survival, including pancreatic cancer, making FAK an excellent target for anti- cancer therapy. Recently, a novel small molecule autophosphorylation FAK inhibitor (1,2,4,5- Benzenetetraamine tetrahydrochloride) called Y15 has been developed by our group that directly and specifically decreased FAK autophosphorylation in vitro and significantly inhibited pancreatic tumor growth in vivo.Y15 inhibitor has a novel mechanism of action; its advantage over existing therapeutic approaches is that that it targets the autophosphorylation site (Y397) of FAK. Y15 is highly specific and non-toxic. The objective of the proposal is to synthesize