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 computational studies and the synthesis and of a variety of non-peptide inhibitors of oncoprotein Bcl-2. Recently, we have disclosed efficient protocols leading to the synthesis of carbazate and dithiocarbazate peptidiomimetics, respectively. This study is now being extended to the synthesis of other<i> </i>analogs 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.

Synthesis and computational studies of peptidomimetics as potential anticancer agents

2019 Spring National Meeting

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