The CXCR4 and CCR5 co-receptors have been revealed as the entry route for HIV into cells, generating interest in a new treatment via fusion inhibitor drugs. CXCR4 expression has also been seen in at least 23 different cancers. Due to biomedical applications, our aim is to develop new antagonists for the CXCR4 co-receptor. Our objectives were to synthesize C3-symmetric tris-linked analogues of our most effective bis-tetraazamacrocycle metal complexes and to characterize their chemical/physical properties in preparation for determining if the added macrocycle enhances their antagonism of CXCR4. Synthetic routes extending our bis-linked ligand syntheses were developed. Metal complexes were made using our previous methods. Various characterization methods were used. C3-symmetric tri-linked bridged tetraazamacrocycles are easily produced. The resulting complexes will inform our understanding of the requirements for producing even more efficient CXCR4 antagonists of this class.

Development in potential anti-HIV and antimetastatic drug: C<sub>3</sub>-symmetric tris-linked bridged tetraazamacrocycles as potential CXCR4 antagonists

243rd National Meeting (2012)

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Development in potential anti-HIV and antimetastatic drug: C3-symmetric tris-linked bridged tetraazamacrocycles as potential CXCR4 antagonists

Development in potential anti-HIV and antimetastatic drug: C₃-symmetric tris-linked bridged tetraazamacrocycles as potential CXCR4 antagonists