Effect of substitution in aryl substituent

February 29, 2024

• Title:       

   Effect of substitution in aryl substituent 

• Image Source:

  Hit generation and exploration: Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases

• Mark:

  Table 3

• Associated context:

  Investigation of the positional effect of the NMe2 substituent revealed that the para-isomer (compound 4) was a  slightly more potent inhibitor of the enzyme than the  meta-isomer 10, and both are significantly more potent  than the ortho-isomer 11. A similar trend was observed  with the OMe substituent (Table 3, compounds 12–  14). In addition to OMe, pyrrolidin-1-yl and pyrid-2-yl  substituents were well tolerated (Table 3, compounds  12, 15, 16).