Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors

Alex G. Waterson; Kirk L. Stevens; Michael J. Reno; Yue Mei Zhang; Eric E. Boros; Frederic Bouvier; Abdullah Rastagar; David E. Uehling; Scott H. Dickerson; Bryan Reep; Octerloney B. McDonald; Edgar R. Wood; David W. Rusnak; Krystal J. Alligood; Sharon K. Rudolph

doi:10.1016/j.bmcl.2006.01.111

Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors

Alex G. Waterson
, Kirk L. Stevens
, Michael J. Reno
, Yue Mei Zhang
, Eric E. Boros
, Frederic Bouvier
, Abdullah Rastagar
, David E. Uehling
, Scott H. Dickerson
, Bryan Reep
, Octerloney B. McDonald
, Edgar R. Wood
, David W. Rusnak
, Krystal J. Alligood
, Sharon K. Rudolph

Cooperative Programs for the Advancement of Earth System Science

Research output: Contribution to journal › Article › peer-review

26 Scopus citations

Abstract

Anilinoalkynylpyrimidines were prepared and evaluated as dual EGFR/ErbB2 kinase inhibitors. A preference was found for substituted phenyl and heteroaromatic rings attached to the alkyne. In addition, the presence of a potential hydrogen bond donor appended to this ring was favored. Selected molecules in the series demonstrated some activity against human tumor cell lines.

Original language	English
Pages (from-to)	2419-2422
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	9
DOIs	https://doi.org/10.1016/j.bmcl.2006.01.111
State	Published - May 1 2006

Keywords

EGFR
ErbB2
Kinase inhibition
Medicinal chemistry
Receptor tyrosine kinase

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10.1016/j.bmcl.2006.01.111

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Waterson, A. G., Stevens, K. L., Reno, M. J., Zhang, Y. M., Boros, E. E., Bouvier, F., Rastagar, A., Uehling, D. E., Dickerson, S. H., Reep, B., McDonald, O. B., Wood, E. R., Rusnak, D. W., Alligood, K. J., & Rudolph, S. K. (2006). Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors. Bioorganic and Medicinal Chemistry Letters, 16(9), 2419-2422. https://doi.org/10.1016/j.bmcl.2006.01.111

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title = "Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors",

abstract = "Anilinoalkynylpyrimidines were prepared and evaluated as dual EGFR/ErbB2 kinase inhibitors. A preference was found for substituted phenyl and heteroaromatic rings attached to the alkyne. In addition, the presence of a potential hydrogen bond donor appended to this ring was favored. Selected molecules in the series demonstrated some activity against human tumor cell lines.",

keywords = "EGFR, ErbB2, Kinase inhibition, Medicinal chemistry, Receptor tyrosine kinase",

author = "Waterson, \{Alex G.\} and Stevens, \{Kirk L.\} and Reno, \{Michael J.\} and Zhang, \{Yue Mei\} and Boros, \{Eric E.\} and Frederic Bouvier and Abdullah Rastagar and Uehling, \{David E.\} and Dickerson, \{Scott H.\} and Bryan Reep and McDonald, \{Octerloney B.\} and Wood, \{Edgar R.\} and Rusnak, \{David W.\} and Alligood, \{Krystal J.\} and Rudolph, \{Sharon K.\}",

year = "2006",

month = may,

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doi = "10.1016/j.bmcl.2006.01.111",

language = "English",

volume = "16",

pages = "2419--2422",

journal = "Bioorganic and Medicinal Chemistry Letters",

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AU - Waterson, Alex G.

AU - Stevens, Kirk L.

AU - Reno, Michael J.

AU - Zhang, Yue Mei

AU - Boros, Eric E.

AU - Bouvier, Frederic

AU - Rastagar, Abdullah

AU - Uehling, David E.

AU - Dickerson, Scott H.

AU - Reep, Bryan

AU - McDonald, Octerloney B.

AU - Wood, Edgar R.

AU - Rusnak, David W.

AU - Alligood, Krystal J.

AU - Rudolph, Sharon K.

PY - 2006/5/1

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N2 - Anilinoalkynylpyrimidines were prepared and evaluated as dual EGFR/ErbB2 kinase inhibitors. A preference was found for substituted phenyl and heteroaromatic rings attached to the alkyne. In addition, the presence of a potential hydrogen bond donor appended to this ring was favored. Selected molecules in the series demonstrated some activity against human tumor cell lines.

AB - Anilinoalkynylpyrimidines were prepared and evaluated as dual EGFR/ErbB2 kinase inhibitors. A preference was found for substituted phenyl and heteroaromatic rings attached to the alkyne. In addition, the presence of a potential hydrogen bond donor appended to this ring was favored. Selected molecules in the series demonstrated some activity against human tumor cell lines.

KW - EGFR

KW - ErbB2

KW - Kinase inhibition

KW - Medicinal chemistry

KW - Receptor tyrosine kinase

UR - https://www.scopus.com/pages/publications/33644974478

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DO - 10.1016/j.bmcl.2006.01.111

M3 - Article

C2 - 16483772

AN - SCOPUS:33644974478

SN - 0960-894X

VL - 16

SP - 2419

EP - 2422

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 9

ER -

Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors

Abstract

Keywords

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