Cathepsin D is an aspartyl protease similar to the HIV-1 aspartyl protease in substrate specificity. Cathepsin D has emerged in recent years as a prognostic indicator in several types of carcinoma, including bladder cancer, colorectal cancer, breast cancer and lung cancer. Also, cathepsin D has been associated with the development of Alzheimer’s disease. Therefore, protease inhibitors can lead to the development of therapeutic agents for treatment of many types of carcinomas and Alzheimer’s disease. Specific proteinase could lead to the development of therapeutic agents for treatment of many types of carcinomas. Described is the design and synthesis of inhibitors containing substituted hydroxyethyl morpholine and substituted hydroxyethyl piperazine isosteres. The synthetic compounds were evaluated as cathepsin D inhibitors by fluorometric assay using as substrate: Ac-Glu-Glu(Edans)-Lys-Pro-Ile-Cys-Phe-Phe-Arg-Leu-Gly-Lys(Methyl Red)-Glu-NH<sub>2</sub>.

Development and screening of new cathepsin D inhibitors

253rd National Meeting (2017)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.