The affinity of RSK for cylitol analogues of SL0101 is critically dependent on the B-ring -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′ hydro...

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Published in:Chemical communications (Cambridge, England) England), 2020-03, Vol.56 (2), p.358-36
Main Authors: Li, Yu, Seber, Pedro, Wright, Eric B, Yasmin, Sharia, Lannigan, Deborah A, O'Doherty, George A
Format: Article
Language:English
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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. The de novo asymmetric synthesis of carbohydrates for the SAR-study of the anticancer natural product, SL0101.
ISSN:1359-7345
1364-548X
DOI:10.1039/d0cc00128g