Search: onr:"swepub:oai:DiVA.org:uu-201387" >
Azastilbenes :
Azastilbenes : a cut-off to p38 MAPK inhibitors
-
- Poon, Jia-Fei (author)
- Uppsala universitet,Syntetisk organisk kemi
-
Alao, John Patrick (author)
-
Sunnerhagen, Per (author)
-
show more...
-
- Dinér, Peter (author)
- Uppsala universitet,Syntetisk organisk kemi
-
show less...
-
(creator_code:org_t)
- 2013
- 2013
- English.
-
In: Organic and biomolecular chemistry. - 1477-0520 .- 1477-0539. ; 11:27, s. 4526-4536
- Related links:
-
https://urn.kb.se/re...
-
show more...
-
https://doi.org/10.1...
-
show less...
Abstract
Subject headings
Close
- Inhibitors with vicinal 4-fluorophenyl/4-pyridine rings on a five- or six-membered heterocyclic ring are known to inhibit the p38 mitogen-activated protein kinase (MAPK), which is a potential target for rheumatoid arthritis and several different types of cancer. Several substituted azastilbene-based compounds with vicinal 4-fluorophenyl/4-pyridine rings were designed using computational docking, synthesized, and evaluated in a cell-free radiometric p38[small alpha] assay. The biochemical evaluation shows that the best inhibition (down to 110 nM) is achieved for azastilbene-based compounds having an isopropylamine substituent in the 2-position of the pyridine ring. The inhibition of p38 signaling in human breast cancer cells was observed for two of the compounds.
Subject headings
- NATURVETENSKAP -- Kemi -- Organisk kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences -- Organic Chemistry (hsv//eng)
Keyword
- Medicinal Chemistry
- Läkemedelskemi
Publication and Content Type
- ref (subject category)
- art (subject category)
Find in a library
To the university's database