Novel 3-alkoxy-1H-pyrazolo[3,4-d]pyrimidines as EGFR and erbB2 receptor tyrosine kinase inhibitors

被引：77

作者：

Ducray, Richard ^{[1
]}

Ballard, Peter ^{[2
]}

Barlaam, Bernard C. ^{[1
]}

Hickinson, Mark D. ^{[2
]}

Kettle, Jason G. ^{[2
]}

Ogilvie, Donald J. ^{[2
]}

Trigwell, Catherine B. ^{[2
]}

机构：

[1] ZI Pompelle, Ctr Rech, AstraZeneca, F-51689 Reims 2, France

[2] AstraZeneca, Canc & Infect Res, Macclesfield SK10 4TG, Cheshire, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 03期

关键词：

pyrazolopyrimidines; erbB2; receptor tyrosine kinase;

D O I：

10.1016/j.bmcl.2007.12.035

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Novel 4-anilino-1H-pyrazolo[3,4-d]pyrimidines have been synthesized and evaluated in vitro for erbB2 and EGFR kinase inhibition. A representative compound displaying oral bioavailability in rat and dog illustrates the potential of this series to provide orally active erbB2 inhibitors. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：959 / 962

页数：4

共 17 条

[1]

5-Substituted 4-anilinoquinazolines as potent, selective and orally active inhibitors of erbB2 receptor tyrosine kinase [J].

Ballard, P ;

Bradbury, RH ;

Hennequin, LFA ;

Hickinson, DM ;

Johnson, PD ;

Kettle, JG ;

Klinowska, T ;

Morgentin, R ;

Ogilvie, DJ ;

Olivier, A .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (19) :4226-4229

[2]

HEIZ2-Positive breast cancer - Current and future treatment strategies [J].

Engel, Ryan H. ;

Kaklamani, Virginia G. .

DRUGS, 2007, 67 (09) :1329-1341

[3]

ERBB receptors and cancer: The complexity of targeted inhibitors [J].

Hynes, NE ;

Lane, HA .

NATURE REVIEWS CANCER, 2005, 5 (05) :341-354

[4]

JANI JP, 2000, CANCER RES, V67, P9887

[5]

The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer [J].

Lippa, Blaise ;

Kauffman, Goss S. ;

Arcari, Joel ;

Kwan, Tricia ;

Chen, Jinshan ;

Hungerford, William ;

Bhattacharya, Samit ;

Zhao, Xumiao ;

Williams, Courtney ;

Xiao, Jun ;

Pustilnik, Leslie ;

Su, Chunyan ;

Moyer, James D. ;

Ma, Ling ;

Campbell, Mary ;

Steyn, Stefanus .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (11) :3081-3086

[6]

CYANOCARBON CHEMISTRY .4. DICYANOKETENE ACETALS [J].

MIDDLETON, WJ ;

ENGELHARDT, VA .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1958, 80 (11) :2788-2794

[7]

CYANOCARBON CHEMISTRY .8. HETEROCYCLIC COMPOUNDS FROM TETRACYANOETHYLENE [J].

MIDDLETON, WJ ;

ENGELHARDT, VA ;

FISHER, BS .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1958, 80 (11) :2822-2829

[8]

Lapatinib [J].

Moy, Beverly ;

Kirkpatrick, Peter ;

Kar, Santwana ;

Goss, Paul .

NATURE REVIEWS DRUG DISCOVERY, 2007, 6 (06) :431-432

[9]

NEIDLEIN R, 1988, SYNTHESIS-STUTTGART, P981

[10]

Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase [J].

Rabindran, SK ;

Discafani, CM ;

Rosfjord, EC ;

Baxter, M ;

Floyd, MB ;

Golas, J ;

Hallett, WA ;

Johnson, BD ;

Nilakantan, R ;

Overbeek, E ;

Reich, MF ;

Shen, R ;

Shi, XQ ;

Tsou, HR ;

Wang, YF ;

Wissner, A .

CANCER RESEARCH, 2004, 64 (11) :3958-3965

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