CAS: 450368-25-9; 2-(Phenylamino)-5-Pyrimidinecarboxylic Acid

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(5-bromo-pyrimidin-2-yl)-phenyl-amine ethyl 2-(phenylamino)pyrimidine-5-carboxylate N-(2-methyl-5-((4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)phenyl)-2-(phenylamino)pyrimidine-5-carboxamide

📜(5-溴嘧啶-2-基)苯胺置于水,Palladium Diacetate,三乙胺,4,5-双二苯基膦-9,9-二甲基氧杂蒽,Lithium Hydroxide体系中,用 四氢呋喃,甲醇,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 15.0H,反应生成 2-苯胺嘧啶-5-羧酸
参考文献:Identification And Optimization Of New Dual Inhibitors Of B-Raf And Epidermal Growth Factor Receptor Kinases For Overcoming Resistance Against Vemurafenib
标题:Identification And Optimization Of New Dual Inhibitors Of B-Raf And Epidermal Growth Factor Receptor Kinases For Overcoming Resistance Against Vemurafenib
摘要:Epidermal Growth Factor Receptor (Egfr) Amplification Has Been Demonstrated To Be Critical For The Inherent And/or Acquired Resistance Against Current B-Raf(V600E) Inhibitor Therapy For Melanoma And Colorectal Cancer Patients. We Describe The Discovery And Structure-Activity Relationship Study Of A Series Of 1H-Pyrazolo[3,4-B]Pyridine-5-Carboxamide Analogues As Novel Dual Inhibitors Of Egfr And B-Raf(V600E) Mutant. One Of The Most Promising Compounds,6A,Potently Inhibited Both Of The Kinases With Ic50 Values Of 8.0 And 51 Nm,Respectively. The Compound Also Strongly Suppressed The Proliferation Of A Panel Of Intrinsic And Acquired Resistant Melanoma And/or Colorectal Cancer Cells Harboring Overexpressed Egfr With Submicromolar Ic50 Values. Further Mechanism Investigation Revealed That 6A Could Sustainably Inhibit The Activation Of The Mapk Path Way In The Resistant Sk-Mel-28 Pr30 Melanoma Cancer Cells And Widr Colorectal Cancer Cells With Egfr Amplification. Our Results Support The Hypothesis That The Egfr/b-Raf(V600E) Dual Inhibition Might Be A Tractable Strategy To Overcome The Intrinsic And Acquired Resistance Of Melanoma And/or Colorectal Cancers Against The Current B-Raf(V600E) Inhibitor Therapy.
DOI:10.1021/jm500007H