CAS: 1152131-73-1; 5-(4-((3-Chloro-4-((3-Fluorobenzyl)Oxy)Phenyl)Amino)Quinazolin-6-yl)Furan-2-Carboxylic Acid

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5-boronofuran-2-carboxylic acid N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-iodoquinazolin-4-amine 3-chloro-4-(3-fluorobenzyloxy)nitrobenzene 6-iodo-1H-quinazolin-4-one 5-{4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl}furan-2-carboxylic acid (tetrahydropyran-2-yloxy)amide 5-{4-[3-chloro-4-(3-fluorobenzyloxy)phenylamino]quinazolin-6-yl}furan-2-carboxylic acid hydroxyamide hydr°Chloride 5-{4-[3-chloro-4-(3-fluorobenzyloxy)phenylamino]quinazolin-6-yl}furan-2-carboxylic acid (2-aminophenyl)amide N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-6-(5-(((4-hydroxybutyl)amino)methyl)-2-furyl)-4-quinazolinamine

📜4-氯-6-碘喹唑啉置于bis(Triphenylphosphine)Palladium(II) Dichloride,Sodium Carbonate体系中,用 乙二醇二甲醚,乙醇,水 用作溶剂,化学反应 1.0H,反应生成拉帕替尼杂质10
参考文献:Novel Chimeric Histone Deacetylase Inhibitors: A Series Of Lapatinib Hybrides As Potent Inhibitors Of Epidermal Growth Factor Receptor (Egfr),Human Epidermal Growth Factor Receptor 2 (Her2),And Histone Deacetylase Activity
标题:Novel Chimeric Histone Deacetylase Inhibitors: A Series Of Lapatinib Hybrides As Potent Inhibitors Of Epidermal Growth Factor Receptor (Egfr),Human Epidermal Growth Factor Receptor 2 (Her2),And Histone Deacetylase Activity
摘要:Reversible Lysine-Specific Acetylation Has Been Described As An Important Posttranslational Modification,Regulating Chromatin Structure And Transcriptional Activity In The Case Of Core Histone Proteins. Histone Deacetylases (Hdac) Are Considered As A Promising Target For Anticancer Drug Development,With 2A As Pan-Hdac Inhibitor Approved For Cutanous T-Cell Lymphoma Therapy And Several Other Hdac Inhibitors Currently In Preclinical And Clinical Development. Protein Kinases Are A Well-Established Target For Cancer Therapy With The Egfr/her2 Inhibitor 5 Approved For Treatment Of Advanced,Her2 Positive Breast Cancer As A Prominent Example. In The Present Report,We Present A Novel Strategy For Cancer Drug Development By Combination Of Egfr/her2 Kinase And Hdac Inhibitory Activity In One Molecule. By Combining The Structural Features Of 5 With An (E)-3-(Aryl)-N-Hydroxyacrylamide Motif Known From Hdac Inhibitors Like 1 Or 3,We Obtained Selective Inhibitors For Both Targets With Potent Cellular Activity (Target Inhibition And Cytotoxicity) Of Selected Compounds 6A And 6C. By Combining Two Distinct Pharmacologically Properties In One Molecule,We Postulate A Broader Activity Spectrum And Less Likelihood Of Drug Resistance In Cancer Patients.
Doi:10.1021/jm100665Z