Title of article :
Synthesis and biological evaluation of benzamides and benzamidines: structural requirement of a pyrimidine ring for inhibition of EGFR tyrosine kinase
Author/Authors :
Toru Asano، نويسنده , , Tomohiro Yoshikawa، نويسنده , , Hiroyuki Nakamura، نويسنده , , Yoshimasa Uehara، نويسنده , , Yoshinori Yamamoto، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2004
Pages :
4
From page :
2299
To page :
2302
Abstract :
The benzamides 1 and the benzamidines 2–3 were synthesized as the mimics of 4-anilinoquinazolines, which possess inhibition of epidermal growth factor receptor (EGFR) tyrosine kinase, and tested for cytotoxicity toward A431 and inhibitory activity toward autophosphorylation by the enzyme assay. High cell growth inhibition was observed in a series of the cyclic benzamides 3: the IC50 values are 0.09–0.32 mM. The benzamidines 3a and 3b exhibited high inhibition of EGFR tyrosine kinase at a 1.0 μM concentration, although the benzamides 1 and the benzamidines 2 did not show significant kinase inhibition at a 10 μM concentration.
Keywords :
EGFR , inhibitor , Benzamidines , Tyrosine kinase.* Corresponding author. Tel.: +81-339860221 , fax: +81-359921029 , e-mail: hiroyuki.nakamura@gakushuin.ac.jp
Journal title :
Bioorganic & Medicinal Chemistry Letters
Serial Year :
2004
Journal title :
Bioorganic & Medicinal Chemistry Letters
Record number :
794387
Link To Document :
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