The affinity of RSK for cylitol analogues of SL0101 is critically dependent on the B-ring C-4'-hydroxy

Five cyclitol analogues of SL0101 with variable substitution at the C-4' position (i.e., OH, Cl, F, H, OMe) were synthesized. The series of analogues were evaluated for their ability to inhibit p90 ribosomal S6 kinase (RSK) activity. The study demonstrated the importance of the B-ring C-4'...

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Published in:Chemical communications (Cambridge, England) England), 2020-03, Vol.56 (20), p.3058-3060
Main Authors: Li, Yu, Seber, Pedro, Wright, Eric B, Yasmin, Sharia, Lannigan, Deborah A, O'Doherty, George A
Format: Article
Language:English
Subjects:
Kinases
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Summary:Five cyclitol analogues of SL0101 with variable substitution at the C-4' position (i.e., OH, Cl, F, H, OMe) were synthesized. The series of analogues were evaluated for their ability to inhibit p90 ribosomal S6 kinase (RSK) activity. The study demonstrated the importance of the B-ring C-4' hydroxy group for RSK1/2 inhibition.
ISSN:1359-7345
1364-548X
DOI:10.1039/d0cc00128g