Practical approach to N-benzyl derivatives of 2-amino-8-methoxy-4H-chromene-3-carbonitrile by reductive amination: Exploration of their effects against protein kinases and in silico ADME profiling
Résumé
The synthesis of 2-benzylamino-8-methoxy-4 H-chromene-3-carbonitriles 7(a-e) has been realized in four steps, via reductive amination from the 2-amino-8-methoxy-4 H-chromene-3-carbonitrile 4 as key intermediate platform with para-and meta-substituted benzaldehydes 5(a-e) , in good overall yields. The physicochemical properties of 7(a-e) and also their aldimines 6(a-e) precursors have been determined using the Swiss ADME server platform according to the Lipinski's descriptors. Biological assays with a panel of six protein kinases such as Hs CDK5-p25, Hs CDK9/cyclin T, Hs Pim1, Hs Haspin, Ssc GSK-3a/ β and Ssc CK1 δ/ ε showed that aldimines 6(a,b) and 6e are potentially interesting because they showed good percentage of residual activities against Hs Pim1 and Hs Haspin.
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Dhiabi et al. - 2022 - Practical approach to N-benzyl derivatives of 2-am.pdf (1.39 Mo)
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Dhia_1-s2.0-S002228602201969X-mmc1.pdf (1.8 Mo)
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