Off-campus WSU users: To download campus access dissertations, please use the following link to log into our proxy server with your WSU access ID and password, then click the "Off-campus Download" button below.
Non-WSU users: Please talk to your librarian about requesting this dissertation through interlibrary loan.
Date of Award
Jeremy J. Kodanko
Photocaging biologically active molecules hold great promise for providing researchers the ability to target key physiological sites in living organisms. This dissertation focuses on improving the efficacy of cysteine cathepsin inhibitors and on the application of inhibitors to be used in novel combination therapies for cancer. Four research areas pertaining to this dissertation, i) Cysteine cathepsin proteases, ii) Cancer treatment, iii) Phototherapy, and iv) Photocages in biological applications were summarized in the introductory chapter. Next, examination of the effect of the steric bulk on Ru(TPA) complexes is described for improving quantum yield of ligand exchange. It showcased that steric bulk accelerates thermal dissociation along with photodissociation. Also, the result presented here show that the metal complexation ameliorates cysteine cathepsins inhibitor efficiency. Later in this thesis, the synthesis and evaluation of a cysteine cathepsin inhibitor-based drug are reported. The inhibitor showcased promising in vitro results as an effective agent to block aberrant proteases and kill cancer cells effectively. Finally, CA-074, a known cathepsin B inhibitor, was caged using bodipy an organic photocage to convert cell impermeable compounds to cell-permeable pro-drugs.
Arora, Karan, "Synthesis, Characterization, Computational & Biological Evaluation Of Caged Bioactive Molecules" (2018). Wayne State University Dissertations. 2006.