7752-74-1Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase inhibitors
Mao, Yongjun,Zhu, Wenxiu,Kong, Xiaoguang,Wang, Zhen,Xie, Hua,Ding, Jian,Terrett, Nicholas Kenneth,Shen, Jingkang
, p. 3090 - 3104 (2013/07/11)
36 new compounds with the typical skeleton of 4-anilino-5-vinyl/ethynyl pyrimidine, 4-anilino-3-cyano-5-vinyl/ethynyl/phenyl pyridine, and m-amino-N-phenylbenzamide, are designed, synthesized and selectively tested on EGFR, ErbB-2 kinases, and A-549, HL60 cells growth inhibition. Results from the bioactivity and chemical structures yield preliminary structure-activity relationships (SARs). The most potent 5-ethynylpyrimidine derivative 20a has an IC50 value of 45 nM to EGFR kinase. Several compounds of other series also show IC50 values 1 μM for EGFR and 5 μM for A-549 and HL60 cells growth inhibition.
5-Alkynyl-pyridines
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, (2013/03/26)
This invention relates to 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of PI3Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification
NEW 5-ALKYNYL-PYRIDINES
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, (2013/03/26)
5-alkynyl-pyridine of general formula (I) which are inhibitors of the activity of PI3K alpha, and their use in the treatment of diseases characterized by excessive or abnormal cell proliferation, such as cancer.
5-ALKYNYL-PYRIMIDINES
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, (2012/02/06)
The present invention encompasses compounds of general formula (1) wherein R1 to R4 R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
NEW 5-ALKYNYL-PYRIDINES
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, (2012/08/08)
This invention relates to 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of PI3Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.
NEW 5-ALKYNYL-PYRIDINES
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, (2012/08/08)
This invention relates to 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of P13Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.
5-ALKYNYL PYRIMIDINES AND THEIR USE AS KINASE INHIBITORS
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Page/Page column 22, (2011/08/21)
The present invention encompasses compounds of general formula (1) wherein R1 to R4 R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors
Suzuki, Naoyuki,Shiota, Takeshi,Watanabe, Fumihiko,Haga, Norihiro,Murashi, Takami,Ohara, Takafumi,Matsuo, Kenji,Oomori, Naoki,Yari, Hiroshi,Dohi, Keiji,Inoue, Makiko,Iguchi, Motofumi,Sentou, Jyunko,Wada, Tooru
scheme or table, p. 1601 - 1606 (2011/05/11)
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).
