CAS: 754214-42-1; 1H-Pyrrolo[2,3-B]Pyridine-5-Carboxylic Acid

该化合物是一种环状环状系统,其特点是有引信的火花和环系统的热循环有机化合物;该化合物的特点是在5个烟花环的定位处有一个箱式酸性功能组,它有助于其酸性;它通常在室温中呈现一种固态,并且由于存在箱状酸组而溶于极地溶液中;该化合物对医药化学和药物开发感兴趣,经常对其潜在的生物活动进行调查,包括防炎和抗癌特性;其分子结构允许进行各种化学修改,这可以加强其药理学特征;此外,环状结构中氮原子的存在会影响其反应和与生物目标的相互作用;它与许多电子外生循环一样,也可能表现出独特的电子特性,使它成为材料科学和有机电子学的一个对象;应当观察安全数据并处理预防措施,如同与所有化学物质一样,以确保实验室的安全做法.

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    📜甲基1H-吡咯并[2,3-B]吡啶-5-甲酸酯置于水,Lithium Hydroxide体系中,用 四氢呋喃,甲醇 作为反应溶剂,化学反应 3.0H,反应生成 7-氮杂吲哚-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

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    专利信息


    专利号:US-7652137-B2
    优先权日:2003-03-06
    标 题:Synthesis of 5 substituted 7-azaindoles and 7-azaindolines
    发明人：GRACZYK PIOTR PAWEL; KHAN AFZAL; BHATIA GURPREET SINGH
    权利人:EISAI R&D MAN CO LTD
    摘要:The present invention provides a novel substituted azaindoline intermediate of formula (I) and a method for its synthesis. The novel substitued azaindoline intermediate (I) is provided for use in the manufacture of 5-substituted 7-azaindolines and 5-substituted 7-azaindoles.

    专利号:ES-2355726-T3
    优先权日:2003-03-06
    标题:SYNTHESIS OF 7-AZAINDOLES AND 7-AZAINDOLINAS REPLACED IN POSITION 5.

    专利号:EP-1633750-A2
    优先权日:2003-03-06
    标 题 :Synthesis of 5-substituted 7-azaindoles and 7-azaindolines

    专利号:WO-2004078757-A2
    优先权日:2003-03-06
    标题:Synthesis of 5-substituted 7-azaindoles and 7-azaidonines

    专利号:JP-2006520771-A
    优先权日:2003-03-06
    标题 :Synthesis of 5-substituted 7-azaindoles and 7-azaindolines

    专利号:EP-1633750-B1
    优先权日:2003-03-06
    标题 :Synthesis of 5-substituted 7-azaindoles and 7-azaindolines

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