EGFR (ErbB1) Inhibitor
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EGFR (ErbB1) Inhibitor


Potent inhibitor of Epidermal growth factor receptor erbB1 with IC50 = 577 nM.


OTAVAchemicals Catalogue Number:   0108440188

CAS Registry Number:  N/A

Purity: 100%

Ref.: Rewcastle et al.  Tyrosine Kinase Inhibitors.  5.  Synthesis and Structure-Activity Relationships  for 4-[(Phenylmethyl)amino]-  and 4-(Phenylamino)quinazolines  as Potent Adenosine 5'-Triphosphate Binding Site Inhibitors of the Tyrosine Kinase Domain of the Epidermal Growth Factor Receptor J. Med. Chem. (1996), 38,  3482-3487

Abstract: A series of 4-substituted quinazolines and related compounds  have been prepared and evaluated for their ability to inhibit the tyrosine kinase activity of the epidermal growth factor receptor on a phospholipase C-gamma 1-derived substrate. The results  show a narrow structure-activity relationship (SAR)  for the basic ring system, with quinazoline being the  preferred chromophore and benzylamino and anilino the preferred side chains.  In the 4-anilino  series, substitution on the 3-position of the phenyl ring with small  lipophilic electron-withdrawing groups provided analogues with enhanced potency.  Two series of compounds  [4-(phenylmethyl)amino and 4-(3-bromophenyl)amino] were studied  to determine SAFb for quinazoline substituents.  In  the more active  4-(3-bromophenyl)amino series,  electron-donating  groups  (NH2, OMe)  at  the  6-  or 7-position  increased activity, in a pattern consistent with a requirement  for high electron density in the vicinity of  the 8-position of  the quinazoline ring.  The 6,7-dimethoxy derivatives were the most effective  in both series, with the 4-(3-bromophenyl)amino derivative (3)  having an IC50  of  0.029 nM, making it by  far the most potent reported inhibitor  of  the tyrosine kinase activity of  the epidermal growth factor receptor  enzyme.