Fang, Xiong’s team published research in European Journal of Medicinal Chemistry in 2020 | CAS: 1195-59-1

2,6-Pyridinedimethanol(cas: 1195-59-1) belongs to pyridine. The basicity and metallophilic high donor number of these π-deficient systems has long favored them as ligands in metal catalysis. The last decade saw pyridine assume a stronger role as functional group for directed C–H oxidation/activation.Application In Synthesis of 2,6-Pyridinedimethanol

Application In Synthesis of 2,6-PyridinedimethanolIn 2020 ,《Design, synthesis, and biological characterization of a new class of symmetrical polyamine-based small molecule CXCR4 antagonists》 appeared in European Journal of Medicinal Chemistry. The author of the article were Fang, Xiong; Meng, Qian; Zhang, Huijun; Liang, Boqiang; Zhu, Siyu; Wang, Juan; Zhang, Chaozai; Huang, Lina S.; Zhang, Xingquan; Schooley, Robert T.; An, Jing; Xu, Yan; Huang, Ziwei. The article conveys some information:

CXCR4, a well-studied coreceptor of human immunodeficiency virus type 1 (HIV-1) entry, recognizes its cognate ligand SDF-1α (also named CXCL12) which plays many important roles, including regulating immune cells, controlling hematopoietic stem cells, and directing cancer cells migration. These pleiotropic roles make CXCR4 an attractive target to mitigate human disorders. Here a new class of sym. polyamines was designed and synthesized as potential small mol. CXCR4 antagonists. Among them, a representative compound 21 (namely HF50731) showed strong CXCR4 binding affinity (mean IC50 = 19.8 nM) in the CXCR4 competitive binding assay. Furthermore, compound 21 significantly inhibited SDF-1α-induced calcium mobilization and cell migration, and blocked HIV-1 infection via antagonizing CXCR4 coreceptor function. The structure-activity relationship anal., site-directed mutagenesis, and mol. docking were conducted to further elucidate the binding mode of compound 21, suggesting that compound 21 could primarily occupy the minor subpocket of CXCR4 and partially bind in the major subpocket by interacting with residues W94, D97, D171, and E288. Our studies provide not only new insights for the fragment-based design of small mol. CXCR4 antagonists for clin. applications, but also a new and effective mol. probe for CXCR4-targeting biol. studies. The results came from multiple reactions, including the reaction of 2,6-Pyridinedimethanol(cas: 1195-59-1Application In Synthesis of 2,6-Pyridinedimethanol)

2,6-Pyridinedimethanol(cas: 1195-59-1) belongs to pyridine. The basicity and metallophilic high donor number of these π-deficient systems has long favored them as ligands in metal catalysis. The last decade saw pyridine assume a stronger role as functional group for directed C–H oxidation/activation.Application In Synthesis of 2,6-Pyridinedimethanol

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