10.1021/jm100576z.s001 Mandy Doering Mandy Doering Lalla A. Ba Lalla A. Ba Nils Lilienthal Nils Lilienthal Carole Nicco Carole Nicco Christiane Scherer Christiane Scherer Muhammad Abbas Muhammad Abbas Abdul Ali Peer Zada Abdul Ali Peer Zada Romain Coriat Romain Coriat Torsten Burkholz Torsten Burkholz Ludger Wessjohann Ludger Wessjohann Marc Diederich Marc Diederich Frederic Batteux Frederic Batteux Marco Herling Marco Herling Claus Jacob Claus Jacob Synthesis and Selective Anticancer Activity of Organochalcogen Based Redox Catalysts American Chemical Society 2010 substrate specificity promise Redox CatalystsMany tumor cells exhibit leukemic cells tumor cell cultures tumor entities animal models micromolar concentrations anticancer activity CLL cells cell lines cancer cells ROS levels reactive oxygen species catalysts act nonmalignant counterparts redox agents PBMC ROS amplification decrease cell proliferation novel organochalcogen carcinoma cell lines intracellular redox state Selective Anticancer Activity tumor initiation chemotherapeutic drugs 2010-10-14 00:00:00 Journal contribution https://acs.figshare.com/articles/journal_contribution/Synthesis_and_Selective_Anticancer_Activity_of_Organochalcogen_Based_Redox_Catalysts/2722018 Many tumor cells exhibit a disturbed intracellular redox state resulting in higher levels of reactive oxygen species (ROS). As these contribute to tumor initiation and sustenance, catalytic redox agents combining significant activity with substrate specificity promise high activity and selectivity against oxidatively stressed malignant cells. We describe here the design and synthesis of novel organochalcogen based redox sensor/effector catalysts. Their selective anticancer activity at submicromolar and low micromolar concentrations was established here in a range of tumor entities in various biological systems including cell lines, primary tumor cell cultures, and animal models. In the B-cell derived chronic lymphocytic leukemia (CLL), for instance, such compounds preferentially induce apoptosis in the cancer cells while peripheral blood mononuclear cells (PBMC) from healthy donors and the subset of normal B-cells remain largely unaffected. In support of the concept of sensor/effector based ROS amplification, we are able to demonstrate that underlying this selective activity against CLL cells are pre-existing elevated ROS levels in the leukemic cells compared to their nonmalignant counterparts. Furthermore, the catalysts act in concert with certain chemotherapeutic drugs in several carcinoma cell lines to decrease cell proliferation while showing no such interactions in normal cells. Overall, the high efficacy and selectivity of (redox) catalytic sensor/effector compounds warrant further, extensive testing toward transfer into the clinical arena.