Synthesis and structure–activity relationships of soluble 8-substituted 4-(2-chlorophenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of the Wee1 and Chk1 checkpoint kinases
Copyright policy )Synthesis and structure–activity relationships of soluble 8-substituted 4-(2-chlorophenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of the Wee1 and Chk1 checkpoint kinases
Pyrrolo[3,4-c]carbazoles bearing solubilising basic side chains at the 8-position retain potent Wee1 and Chk1 inhibitory properties in isolated enzyme assays, and evidence of G2/M checkpoint abrogation in several cellular assays. Co-crystal structure studies confirm that the primary binding to the Wee1 enzyme is as described previously, with the C-8 side chains residing in an area of bulk tolerance.
- Pfizer (United States) United States
- University of Auckland New Zealand
Molecular Structure, Carbazoles, Nuclear Proteins, Cell Cycle Proteins, Protein-Tyrosine Kinases, Structure-Activity Relationship, Checkpoint Kinase 1, Combinatorial Chemistry Techniques, Humans, Protein Kinase Inhibitors, Protein Kinases
Molecular Structure, Carbazoles, Nuclear Proteins, Cell Cycle Proteins, Protein-Tyrosine Kinases, Structure-Activity Relationship, Checkpoint Kinase 1, Combinatorial Chemistry Techniques, Humans, Protein Kinase Inhibitors, Protein Kinases
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