Open AccessThe affinity of RSK for cylitol analogues of SL0101 is critically dependent on the B-ring C-4′-hydroxy
Author(s) -
Yu Li,
Pedro Seber,
Eric B Wright,
Sharia Yasmin,
Deborah A. Lannigan,
George A. O’Doherty
Publication year - 2020
Publication title -
chemical communications
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.837
H-Index - 333
eISSN - 1364-548X
pISSN - 1359-7345
DOI - 10.1039/d0cc00128g
Subject(s) - ring (chemistry) , chemistry , stereochemistry , natural product , combinatorial chemistry , organic chemistry
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.