Synthesis of (Z)-3-((1H-imidazol-5-yl)methylene)indolin-2-one Derivatives as Pim Kinase Inhibitors
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Pim kinases are important targets for hematological cancer therapy because they are involved in key cellular processes such as differentiation, proliferation, survival, apoptosis, and tumorigenesis. Here, inhibitors of Pim kinases were designed and synthesized based on an indolin-2-one scaffold. Introduction of a (1H-imidazol-5-yl)methylenyl group at position 3, a 3-aminopiperidinyl group at position 4, and an amino group at position 5 of indolin-2-one resulted in inhibited Pim kinase activity. Compounds 7a and 7d showed submicromolar IC50 values against all three Pim kinases.
Abstract
Pim kinases are important targets for hematological cancer therapy because they are involved in key cellular processes such as differentiation, proliferation, survival, apoptosis, and tumorigenesis. Here, inhibitors of Pim kinases were designed and synthesized based on an indolin-2-one scaffold. Introduction of a (1H-imidazol-5-yl)methylenyl group at position 3, a 3-aminopiperidinyl group at position 4, and an amino group at position 5 of indolin-2-one resulted in inhibited Pim kinase activity. Compounds 7a and 7d showed submicromolar IC50 values against all three Pim kinases.
참고문헌 (13)
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