2. Academic Validation
  3. Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors

Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors

  • Bioorg Med Chem Lett. 2011 Mar 15;21(6):1601-6. doi: 10.1016/j.bmcl.2011.01.119.
Naoyuki Suzuki 1,  Takeshi Shiota,  Fumihiko Watanabe,  Norihiro Haga,  Takami Murashi,  Takafumi Ohara,  Kenji Matsuo,  Naoki Oomori,  Hiroshi Yari,  Keiji Dohi,  Makiko Inoue,  Motofumi Iguchi,  Jyunko Sentou,  Tooru Wada
Affiliations

Affiliation

  • 1 Shionogi Medicinal Research Laboratories, Shionogi & Co., Ltd, Fukushima-ku, Osaka, Japan. naoyuki.suzuki@shionogi.co.jp
PMID: 21334203 DOI: 10.1016/j.bmcl.2011.01.119
Abstract

A structure-activity relationship study of 4-anilinopyrimidines for dual EGFR/Her-2 inhibitor has resulted in the identification of 4-anilino-5-alkenyl or 5-alkynyl-6-methylpyrimidine derivatives that have exhibited effective inhibitory activity against both Enzymes. The presence of 5-alkenyl or 5-alkynyl moiety bearing terminal hydrophilic group played important role for inhibition of these Enzymes. Selected compounds in the series demonstrated some activity against Her-2 dependent cell line (BT474).

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