Article citationsMore>>

Siedle, B., García-Piñeres, A.J., Murillo, R., Schulte-Mönting, J., Castro, V., Rüngeler, P., Klaas, C.A., Da Costa, F.B., Kisiel, W. and Merfort, I. (2004) Quantitative Structure-Activity Relationship of Sesquiterpene Lactones as Inhibitors of the Transcription Factor NF-κB. Journal of Medicinal Chemistry, 47, 6042-6054.
http://dx.doi.org/10.1021/jm049937r

has been cited by the following article:

• TITLE: Natural and Semi-Synthetic Pseudoguaianolides as Inhibitors of NF-κB

  AUTHORS: Rodrigo Villagomez, Juan Antonio Collado, Eduardo Muñoz, Giovanna Almanza, Olov Sterner

  KEYWORDS: Damsin, α Methylene-γ-Lactone Sesquiterpenoids, Anti-Cancer Activity

  JOURNAL NAME: Journal of Biomedical Science and Engineering, Vol.7 No.10, August 14, 2014

  ABSTRACT: Damsin (1) is a natural pseudoguaianolide sesquiterpene that inhibits NF-κB, a protein complex that controls the transcription of DNA in mammalian cells, and has a potential for standing model for the development of new anti-cancer lead structures. In order to do a preliminary structure-activity study and improve the anti-cancer activity, fourteen derivatives and analogs were prepared and evaluated. These were chosen to represent both structural diversity and structural novelty. The importance of α methylene-γ-lactone moiety for the anti-cancer activity was confirmed, even though other features in the scaffold were shown to be important for the activity. In some cases a new substitution negatively affected the initial activity, however, two analogues, indolo [3,2-c]-4-desoxydamsin (5) and ambrosin (6), were found to be more potent.