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- W1999286871 abstract "The structure–activity relationship (SAR) of 5-substituted pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione derivatives 5 was investigated for their potential as Chk1 inhibitors for possible chemo- and radio-potentiators in anticancer chemotherapies. In silico virtual screening helped to optimize the substituent on the phenyl ring, and led to identification of the m-carbamoyl group among the 117 analogues tested. Further optimization studies focusing on the docking model of 15 in the active site of Chk1 revealed that 32b (IC50 = 2.8 nM) was a more potent inhibitor than UNC-01." @default.
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- W1999286871 date "2010-11-15" @default.
- W1999286871 modified "2023-09-27" @default.
- W1999286871 title "Synthesis and evaluation of 5-substituted 9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as check point 1 kinase inhibitors" @default.
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- W1999286871 doi "https://doi.org/10.1016/j.bmc.2010.09.042" @default.
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