Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593238 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
5-Alkenyl or 5-alkynyl-4-anilinopyrimidines were prepared and evaluated for in vitro inhibition of EGFR/Her-2 kinase activity and the growth of tumor cell lines (BT474 and N87). Several of these compounds inhibited the growth of BT474 and N87 at concentrations below 200Â nM. Structure-activity relationship studies revealed a critical role for the 5-alkynyl moieties. The representative compound 19 exhibited significant antitumor potency in a mouse xenograft model.
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Authors
Naoyuki Suzuki, Takeshi Shiota, Fumihiko Watanabe, Norihiro Haga, Takami Murashi, Takafumi Ohara, Kenji Matsuo, Naoki Omori, Hiroshi Yari, Keiji Dohi, Makiko Inoue, Motofumi Iguchi, Jyunko Sentou, Tooru Wada,