CAS: 63894-67-7; 4-(2-Chlorothieno[2,3-D]Pyrimidin-4-yl)Morpholine

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955978-98-0 1703014-48-5 383146-87-0

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CAS号955978-98-0 2-氯-4-吗啉噻吩并[2,3...

📜在 水,Sodium Hydroxide,三氯氧磷体系中,用 乙醇,乙腈 作为反应溶剂,化学反应 42.33H,反应生成 2-氯-4-吗啡啉基噻吩并[2,3-D]嘧啶
参考文献:Rational Design Of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity Over The Phosphoinositide 3-Kinase β Isoform
标题:Rational Design Of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity Over The Phosphoinositide 3-Kinase β Isoform
摘要:Of The Four Class I Phosphoinositide 3-Kinase (Pi3K) Isoforms,Pi3K Alpha Has Justly Received The Most Attention For Its Potential In Cancer Therapy. Herein We Report Our Successful Approaches To Achieve Pi3K Alpha Vs Pi3K Beta Selectivity For Two Chemical Series. In The Thienopyrimidine Series Of Inhibitors,We Propose That Select Ligands Achieve Selectivity Derived From A Hydrogen Bonding Interaction With Arg770 Of Pi3K Alpha That Is Not Attained With The Corresponding Lys777 Of Pi3K Beta. In The Benzoxepin Series Of Inhibitors,The Selectivity Observed Can Be Rationalized By The Difference In Electrostatic Potential Between The Two Isoforms In A Given Region Rather Than Any Specific Interaction.
DOI:10.1021/jm2007084