Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles

Autor: Edgars Jecs, Yesim A. Tahirovic, Robert J. Wilson, Eric J. Miller, Michelle Kim, Valarie Truax, Huy H. Nguyen, Nicholas S. Akins, Manohar Saindane, Tao Wang, Chi S. Sum, Mary E. Cvijic, Gretchen M. Schroeder, Samantha L. Burton, Cynthia A. Derdeyn, Lingjie Xu, Yi Jiang, Lawrence J. Wilson, Dennis C. Liotta
Rok vydání: 2022
Předmět:
Zdroj: Journal of medicinal chemistry. 65(5)
ISSN: 1520-4804
Popis: Our first-generation CXCR4 antagonist TIQ15 was rationally modified to improve drug-like properties. Introducing a nitrogen atom into the aromatic portion of the tetrahydroisoquinoline ring led to several heterocyclic variants including the 5,6,7,8-tetrahydro-1,6-naphthyridine series, greatly reducing the inhibition of the CYP 2D6 enzyme. Compound
Databáze: OpenAIRE