Design, Synthesis and Biological Evaluation of Chromone-based p38 MAP Kinase Inhibitors
2011 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 54, no 20, 7427-7431 p.Article in journal (Refereed) Published
A series of 3-(4-fluorophenyl)-2-(4-pyridyl)-chromone derivs. were synthesized and evaluated as p38 MAP kinase inhibitors. Introduction of an amino group in the 2-position of the pyridyl moiety gave p38 inhibitors with IC50 values in the low nanomolar range (e.g. 8a; IC50 = 17 nm). Addnl., the inhibitors (8a and 8e) demonstrate an excellent selectivity profile towards the p38 kinase among other kinases, as well as inhibition (8e) of p38 signaling in human breast cancer cells. [on SciFinder(R)]
Place, publisher, year, edition, pages
2011. Vol. 54, no 20, 7427-7431 p.
IdentifiersURN: urn:nbn:se:uu:diva-159363DOI: 10.1021/jm200818jPubMedID: 21905739OAI: oai:DiVA.org:uu-159363DiVA: diva2:444488
written in English2011-09-292011-09-292011-11-04Bibliographically approved