CAS: 221698-39-1; 4-Chloro-6,7-Dimethoxyquinazolin-2-Amine

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2-amino-6,7-dimethoxyquinolizin-4(3H)-one methyl 2-amino-4,5-dimethoxybenzoate

📜2-氨基-4,5-二甲氧基苯甲酸甲酯置于盐酸,三氯氧磷体系中,用 1,4-二氧六环 用作溶剂,化学反应 15.5H,反应生成4-氯-6,7-二甲氧基-喹唑啉-2-胺
参考文献:Tyrosine Kinase Inhibitors. 8. An Unusually Steep Structure−activity Relationship For Analogues Of 4-(3-Bromoanilino)-6,7-Dimethoxyquinazoline (Pd 153035),A Potent Inhibitor Of The Epidermal Growth Factor Receptor
标题:Tyrosine Kinase Inhibitors. 8. An Unusually Steep Structure−activity Relationship For Analogues Of 4-(3-Bromoanilino)-6,7-Dimethoxyquinazoline (Pd 153035),A Potent Inhibitor Of The Epidermal Growth Factor Receptor
摘要:4-(3-Bromoanilino)-6,7-Dimethoxyquinazoline (32,Pd 153035) Is A Very Potent Inhibitor (Ic50 0.025 Nm) Of The Tyrosine Kinase Activity Of The Epidermal Growth Factor Receptor (Egfr),Binding Competitively At The Atp Site. Structure-Activity Relationships For Close Analogues Of 32 Are Very Steep. Some Derivatives Have Ic(50)S Up To 80-Fold Better Than Predicted From Simple Additive Binding Energy Arguments,Yet Analogues Possessing Combinations Of Similar Phenyl And Quinazoline Substituents Do Not Show This ''Supra-Additive'' Effect. Because Some Substituents Which Are Mildly Deactivating By Themselves Can Be Strongly Activating When Used In The Correct Combinations,It Is Proposed That Certain Substituted Analogues Possess The Ability To Induce A Change In The Conformation Of The Receptor When They Bind. There Is Some Bulk Tolerance For Substitution In The 6-And 7-Positions Of The Quinazoline,So That 32 Is Not The Optimal Inhibitor For The Induced Conformation. The Diethoxy Derivative 56 [4-(3-Bromoanilino)-6,7-Diethoxyquinazoline] Shows An Ic50 Of 0.006 Nm,Making It The Most Potent Inhibitor Of The Tyrosine Kinase Activity Of The Egfr Yet Reported.
Doi:10.1021/jm9503613