Towards the Synthesis of New Highly Functionalized Molecular Scaffolds for Peptide Cyclizations
نویسنده
چکیده
5 1. General Introduction: mimicry of protein binding surfaces 6 1.1 Linear versus cyclic peptides 7 1.2 CLIPSTM technology 9 1.3 Aim of the research project 12 2. Results and discussion 15 2.1 Negishi cross-coupling 15 2.2 C-C bond formation via organolithium reagent 19 2.3 C-C bond formation via Gilman reagent 24 2.4 Towards the synthesis of an alternative scaffold 25 3. Conclusions 31 4. Future prospects 33 5. Experimental section 34 6. References 41
منابع مشابه
Design and Synthesis of Novel Triazole-based Peptide Analogues as Anticancer Agents
Cancer disease is a great concern in the worldwide public health and current treatments do not give satisfactory results, so, developing novel therapeutic agents to combat cancer is highly demanded. Nowadays, anticancer peptides (ACPs) are becoming promising anticancer drug candidates. This is due to several advantages inherited in peptide molecules, such as being usually with small size, high ...
متن کاملDesign and Synthesis of Novel Triazole-based Peptide Analogues as Anticancer Agents
Cancer disease is a great concern in the worldwide public health and current treatments do not give satisfactory results, so, developing novel therapeutic agents to combat cancer is highly demanded. Nowadays, anticancer peptides (ACPs) are becoming promising anticancer drug candidates. This is due to several advantages inherited in peptide molecules, such as being usually with small size, high ...
متن کاملOne-pot Synthesis and Characterization of Highly Functionalized Thiazoles
A facile and efficient one-pot three-step process for the synthesis of 5-acetyl-2-imino-4-methylthiazoles via the cyclocondensation of 3-thiocyanatoacetylacetone with various hydrazine or hydrazide derivatives in EtOH has been developed. 3-Thiocyanatoacetylacetone itself has been synthesized as the intermediate from substitution reaction of thiocyanate with 3-chloroacetylacetone. B...
متن کاملHighly diastereoselective samarium diiodide induced cyclizations of new 3-substituted indole derivatives.
Herein, we describe the synthesis of new functionalized tricyclic and tetracyclic indole derivatives via samarium diiodide induced ketyl cyclizations. The intermediate samarium organyls were either protonated using different proton sources or alkylated with various electrophiles in a highly diastereoselective manner. The obtained products were subjected to further transformations leading to syn...
متن کاملSynthesis, Radiolabeling, and Biological Evaluation of Peptide LIKKPF Functionalized with HYNIC as Apoptosis Imaging Agent
Introduction: A noninvasive method of detecting exposure of phosphatidylserine (PS) on the external surface of the plasma membrane such as nuclear imaging could assist the diagnosis and therapy of apoptosis related pathologies. The most studied imaging agent for apoptosis is Annexin V so far. Because of limitations of Annexin V other agents have been introduced such as small peptides and molecu...
متن کامل