Design, synthesis, biological evaluation of novel small molecule inhibitors for early diagnosis and therapy of prostate cancer

Abstract

19.3 million new cancer cases and 10 million cancer deaths are reported worldwide in the year 2020. In the male population, prostate cancer (PCa), is the second most diagnosed cancer. PSMA is a membrane-bound protein and is an important target to identify prostate cancer at an early stage. It is overexpressed 100 to 1000-fold in cancerous tissues than that of the normal or healthy cells. In this study, we have designed ten aminoacetamide-based ligands to target PSMA protein. Molecular docking studies were performed to identify potent ligands, and currently, we are synthesizing the new ligands. The best among the designed ligands will be used in solid phase peptide methodology to synthesize bioconjugates that can be attached to a fluorescent reporter, rhodamine B or chelating moiety to deliver radioisotopes such as 99mTc for early diagnosis of PCa. The bioconjugates have potential applications for performing diagnosis and intraoperative fluorescence-guided surgery (FGS) of PCa.