… A series of six–six and six–five fused heterocyclic CXCR3 antagonists has been synthesized
… properties that could serve as useful tools to study the role of the CXCR3 receptor in vivo. …

… Overall, the examined heterocyclic replacements did not … the heterocyclic replacements were
not adopted for further studies. … to use the 8-azaquinazolinone core for further optimization. …

A series of quinazolinone-derived inhibitors of the CXCR3 receptor have been synthesized
and their affinity for the receptor evaluated. Compounds were evaluated in a 125 I-IP10 …

… Classes of CXCR3 antagonists with strikingly variable core … bicyclic core for a wide
variety of heterocyclic groups (16) was … and optimization of a series of quinazolinone-derived …

… Overall, the examined heterocyclic replacements did not provide any improve- ment in …
In summary, further optimization of the quinazolinone-derived CXCR3 antagonists led to the …

… we explored the benzimidazolo-thiazole core scaffold. The … ring was replaced by smaller
heterocycles. Herein, we describe … We started our optimization program with the replacement of …

… Optimization of the quinazolinone series from which AMG 487 emerged identified a lead …
Similarly, substitution at the C4-position of the azaquinazolinone core also yielded derivatives …

… of the optimized derivative compounds have produced CXCR3 … of two high affinity CXCR3
antagonists were shown, which … nitrogen atoms in the heterocyclic scaffold of the compound …

… Lead optimization with this strategy led to the discovery of compound 14n ( Figure 3 ,
compound 7 ) as the most potent CXCR3 antagonist on both human and mouse CXCR3 inhibiting …

… The CXCR3 antagonist activities were measured in CXCR3 mediated chemotaxis assays …
NCI compounds were docked against the optimized homology model with the MOE docking …