Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors

Abstract Structure–activity relationship (SAR) studies on a highly potent series of arylamide FMS inhibitors were carried out with the aim of improving FMS kinase selectivity, particularly over KIT. Potent compound 17r (FMS IC50 0.7nM, FMS cell IC50 6.1nM) was discovered that had good PK properties...
Ausführliche Beschreibung

Gespeichert in:
Autor*in:

Illig, Carl R. [verfasserIn]

Manthey, Carl L.

Meegalla, Sanath K.

Wall, Mark J.

Chen, Jinsheng

Wilson, Kenneth J.

DesJarlais, Renee L.

Ballentine, Shelley K.

Schubert, Carsten

Crysler, Carl S.

Chen, Yanmin

Molloy, Christopher J.

Chaikin, Margery A.

Donatelli, Robert R.

Yurkow, Edward

Zhou, Zhao

Player, Mark R.

Tomczuk, Bruce E.

Format:

E-Artikel

Sprache:

Englisch

Erschienen:

2013transfer abstract

Schlagwörter:

Rheumatoid arthritis

Colony-stimulating factor-1 receptor

Macrophage colony-stimulating factor

KIT

Hypocellularity

FMS

Anti-inflammatory

Umfang:

7

Übergeordnetes Werk:

Enthalten in: Feeding European sea bass ( - Torrecillas, S. ELSEVIER, 2018, a Tetrahedron publication for rapid dissemination of preliminary communications on all aspects of bioorganic chemistry, medicinal chemistry, bioinorganic chemistry and related disciplines, Amsterdam [u.a.]

Übergeordnetes Werk:

volume:23 ; year:2013 ; number:23 ; day:1 ; month:12 ; pages:6363-6369 ; extent:7

Links:

Volltext

DOI / URN:

10.1016/j.bmcl.2013.09.061

Katalog-ID:

ELV011755504

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