CAS: 149082-03-1; (3,5-Dimethyl-4-Nitropyridin-2-yl)Methanol

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CAS号86604-79-7 4-硝基-2,3,5-三甲基吡... | CAS号695-98-7 2,3,5-三甲基吡啶 | CAS号74409-42-0 2,3,5-三甲基吡啶 N-氧化物

📜2,3,5-三甲基吡啶 1-氧化物置于硫酸,硝酸,Potassium Carbonate体系中,用 甲醇 用作溶剂,化学反应 24.0H,反应生成3,5-二甲基-4-硝基吡啶-2-甲醇
参考文献:Rationally Designed High-Affinity 2-Amino-6-Halopurine Heat Shock Protein 90 Inhibitors That Exhibit Potent Antitumor Activity
标题:Rationally Designed High-Affinity 2-Amino-6-Halopurine Heat Shock Protein 90 Inhibitors That Exhibit Potent Antitumor Activity
摘要:Heat Shock Protein 90 (Hsp90) Is A Molecular Chaperone Protein Implicated In Stabilizing The Conformation And Maintaining The Function Of Many Cell-Signaling Proteins. Many Oncogenic Proteins Are More Dependent On Hsp90 In Maintaining Their Conformation,Stability,And Maturation Than Their Normal Counterparts. Furthermore,Recent Data Show That Hsp90 Exists In An Activated Form In Malignant Cells But In A Latent Inactive Form In Normal Tissues,Suggesting That Inhibitors Selective For The Activated Form Could Provide A High Therapeutic Index. Hence,Hsp90 Is Emerging As An Exciting New Target For The Treatment Of Cancer. We Now Report On A Novel Series Of 2-Amino-6-Halopurine Hsp90 Inhibitors Exemplified By 2-Amino-6-Chloro-9-(4-Iodo-3,5-Dimethylpyridin-2-Ylmethyl)Purine (30). These Highly Potent Inhibitors (Ic50 Of 30 = 0.009 Mu M In A Her-2 Degradation Assay) Also Display Excellent Antiproliferative Activity Against Various Tumor Cell Lines (Ic50 Of 30 = 0.03 Mu M In Mcf7 Cells). Moreover,This Class Of Inhibitors Shows Higher Affinity For The Activated Form Of Hsp90 Compared To Our Earlier 8-Sulfanylpurine Hsp90 Inhibitor Series. When Administered Orally To Mice,These Compounds Exhibited Potent Tumor Growth Inhibition (> 80%) In An N87 Xenograft Model,Similar To That Observed With 17-Allylamino-17-Desmethoxygeldanamycin (17-Aag),Which Is A Compound Currently In Phase I/ii Clinical Trials.
Doi:10.1021/jm050752+

专利信息

专利号:WO-0000474-A1
优先权日:1998-06-26
标题:Pyridine building blocks as intermediates in the synthesis of pharmaceutically active compounds
发明人：NIKOLOPOULOS ANGELO; SCHICKANEDER HELMUT; KOCHER CHRISTIAN; MURPHY TREVOR; HERMANN GESINE
权利人:RUSSINSKY LTD; NIKOLOPOULOS ANGELO; SCHICKANEDER HELMUT; KOCHER CHRISTIAN; MURPHY TREVOR; HERMANN GESINE
摘要:Complexes of formulae (II or III) are useful intermediates for preparing compounds of formula (IV) which in turn may be converted into a pyridine benzimidazole.