Design, Synthesis, and Biological Evaluation of Chromone-Based p38 MAP Kinase Inhibitors | Zendy

Christine Dyrager | Zendy; Linda Nilsson Möllers | Zendy; Linda Karlsson Kjäll | Zendy; John P. Alao | Zendy; Peter Dinér | Zendy; Fredrik K. Wallner | Zendy; Per Sunnerhagen | Zendy; Morten Grøtli | Zendy

AI Assistant Blog Pricing

Home ZAIA Blog

Open Access

Design, Synthesis, and Biological Evaluation of Chromone-Based p38 MAP Kinase Inhibitors

Author(s) -

Christine Dyrager,

Linda Nilsson Möllers,

Linda Karlsson Kjäll,

John P. Alao,

Peter Dinér,

Fredrik K. Wallner,

Per Sunnerhagen,

Morten Grøtli

Publication year - 2011

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm200818j

Subject(s) - chromone , chemistry , moiety , kinase , p38 mitogen activated protein kinases , selectivity , stereochemistry , mitogen activated protein kinase , structure–activity relationship , biochemistry , protein kinase a , in vitro , catalysis

3-(4-Fluorophenyl)-2-(4-pyridyl)chromone derivatives were synthesized and evaluated as p38 MAP kinase inhibitors. Introduction of an amino group in the 2-position of the pyridyl moiety gave p38α inhibitors with IC(50) in the low nanomolar range (e.g., IC(50) = 17 nm). The inhibitors showed excellent selectivity profiles when tested on a panel of 62 kinases, as well as efficient inhibition of p38 signaling in human breast cancer cells.

The content you want is available to Zendy users.

Already have an account? Click here to sign in.

Having issues? You can contact us here

Accelerating Research