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Name Mr. Reed Roberts
Organization or Institution Southeastern University
Presentation Type Poster
Topic Organic Chemistry
Title

Applications of the Cesium Effect: Synthesis of de Novo Peptidomimetics as Potential Anticancer Agents.

Author(s)

Reed W. Roberts, Aaron J. Todman, Quintan T. Rossow, Mark E. Steury, Nathaniel J. Jordan, Lucas Kline and Ralph N. Salvatore*

Author Institution(s)

Southeastern University
Department of Natural Sciences
1000 Longfellow Blvd.
Lakeland, FL, 33801

Abstract

Numerous physiological and pathological stimuli induced programmed cell death (apoptosis), and the Bcl-2 family of oncoproteins plays a central role in this regulation. Proteins such as Bcl-2 are known to inhibit apoptosis, and uncontrolled cell survival due to Bcl-2 overexpression has been proven to make a significant contribution to tumor formation. With this in mind, we have directed our attention toward the synthesis of a variety of non-peptide inhibitors of oncoprotein Bcl-2. Thus, we disclose herein efficient protocols leading to the synthesis of carbazate, dithiocarbazate, dithiocarbamate, a "carbamatoid" and amine peptidomimetics, respectively. This study is now being extended to the synthesis of other de novo analogs (diselenocarbamate) with similar structural features to natural proteins, that may interrupt protein-protein interactions. Utilizing our aforementioned protocols, various scaffoldings are being employed for the development of novel artificial biomolecules, which may result in interesting biological behaviors regarding the disruption of protein-protein interactions and furthermore, may serve as potential therapeutics in clinical chemotherapy.