Article citationsMore>>

Wissner, A., Overbeek, E., Reich, M.F., Floyd, M.B., Johnson, B.D., Mamuya, N., Rosfjord, E.C., Discafani, C., Davis, R., Shi, X., Rabindran, S.K., Gruber, B.C., Ye, F., Hallett, W.A., Nilakantan, R., Shen, R., Wang, Y.-F., Greenberger, L.M. and Tsou, H.R. (2002) Synthesis and Structure-Activity Relationships of 6,7-Disubstituted 4-Anilinoquinoline-3-Carbonitriles. The Design of an Orally Active, Irreversible Inhibitor of the Tyrosine Kinase Activity of the Epidermal Growth Factor Receptor (EGFR) and the Human Epidermal Growth Factor Receptor-2 (HER-2). Journal of Medicinal Chemistry, 46, 49-63.
http://dx.doi.org/10.1021/jm020241c

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.