CAS: 106486-76-4; Azinomycin B

该化合物是属于亚氮素抗生素类化合物的自然产生的抗生素,由细菌链球菌的某些菌株产生,其特点是分子结构复杂,包括独特的双环核心和各种功能组,有助于其生物活动;Aziomicayn B具有强大的抗菌特性,特别是针对模范细菌,并因其抑制DNA合成的能力而研究其在癌症治疗中的潜在用途;该化合物的行动机制涉及干扰核酸新陈代谢,使其成为医学化学的主体;此外,Azinocyn B在研究其对肿瘤细胞的细胞毒性影响方面表现出了希望;其稳定性,溶性和再活性受到结构特征的影响,这些特征对其生物功效至关重要;与许多抗生素一样,抗药性的发展是一个关切问题,它促使人们不断研究其药理特性和可能的治疗应用.

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      专利信息


      专利号:WO-9502566-A1
      优先权日:1993-07-16
      标题 :Synthesis of combinatorial arrays of organic compounds through the use of multiple component combinatorial array syntheses
      发明人:ARMSTRONG ROBERT W
      权利人:UNIV CALIFORNIA; ARMSTRONG ROBERT W
      摘要:The present invention relates to an array of compounds having a common core structure wherein the compounds of the array comprise the products of a multiple component combinatorial array synthesis having at least three components. The present invention also relates to the method of synthesizing that array. A further embodiment of the present invention relates to the use of solid phase synthesis to synthesize the combinatorial array of compounds. The present invention also relates to a method of creating a combinatorial array of compounds with a common core structure by identifying the desired core structure, identifying an MCCA reaction capable of generating that core structure, followed by preparing an array of compounds using the identified MCCA reaction according to the aforementioned method. The present invention also relates to a method for conducting in vitro assays of biological material using the combinatorial arrays of the present invention.

      专利号:US-10472663-B2
      优先权日:2015-01-21
      标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit protein synthesis
      发明人:FERNÃ?NDEZ GARCÃ?A JOSÉ LUIS; GOSÃ?LVEZ BERENGUER JAIME; BOU ARÉVALO GERMÃ?N; TAMAYO NOVAS MARIA; SANTISO BRANDARIZ REBECA; OTERO FARIÑA FÃ?TIMA MARÃ?A
      权利人:ABM TECH LLC
      摘要:The present invention relates to a method for the rapid evaluation of bacterial susceptibility or non-susceptibility of bacteria to antibiotics that inhibit protein synthesis. The rationale is to identify bacterial responses that depend or are influenced by protein synthesis. If this response is prevented or reduced by the antibiotic that inhibits the protein synthesis, the bacteria are susceptible to this antibiotic. Otherwise, if the response keeps similar despite the incubation with the antibiotic, the bacteria are not susceptible or resistant to this antibiotic. These responses could be determined at the DNA lev-el, cell wall level, morphological level or any other experimental approach, including metabolic, bio-chemical, physiological or genetic processes.

      专利号:JP-H09506857-A
      优先权日:1993-07-16
      标 题:Synthesis of combinatorial arrays of organic compounds by multi-component combinatorial array synthesis

      专利号:EP-0708751-A1
      优先权日:1993-07-16
      标题:Synthesis of combinatorial arrays of organic compounds through the use of multiple component combinatorial array syntheses

      专利号:CA-2167391-A1
      优先权日:1993-07-16
      标 题 :Synthesis of combinatorial arrays of organic compounds through the use of multiple component combinatorial array syntheses

      专利号:ES-2710679-T3
      优先权日:2015-01-21
      标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit the synthesis of proteins

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      主要参考文献


      1: Balazy M, Fausto A, Voskanian C, Chavez B, Panesar H, Minehan TG. Dimeric and trimeric derivatives of the azinomycin B chromophore show enhanced DNA binding. Org Biomol Chem. 2017 May 31;15(21):4522-4526. doi: 10.1039/c7ob00944e.
      2: Senthilnathan D, Kalaiselvan A, Venuvanalingam P. Sequence selectivity of azinomycin B in DNA alkylation and cross-linking: a QM/MM study. J Mol Model. 2013 Jan;19(1):383-90. doi: 10.1007/s00894-012-1557-2. Epub 2012 Aug 24. 44(1):187-97. doi: 10.1093/nar/gkv949. Epub 2015 Sep 22.
      4: Zhao Q, He Q, Ding W, Tang M, Kang Q, Yu Y, Deng W, Zhang Q, Fang J, Tang G, Liu W. Characterization of the azinomycin B biosynthetic gene cluster revealing a different iterative type I polyketide synthase for naphthoate biosynthesis. Chem Biol. 2008 Jul 21;15(7):693-705. doi: 10.1016/j.chembiol.2008.05.021. 8(6):1065-8. doi: 10.1021/ol052987l. 7(9):2563-70. doi: 10.1039/c1mb05136a. Epub 2011 Jul 21. 39(48):14968-75. doi: 10.1021/bi001998d. 337(2):147-54. doi: 10.1111/1574-6968.12020. Epub 2012 Nov 2. 13(5):485-92. doi: 10.1016/j.chembiol.2006.02.015. 6(6):1071-81. doi: 10.1039/b926358f. Epub 2010 Mar 16.

      合成参考文献


      参考文献:10.1039/c1mb05136a
      摘要:Foulke-Abel J, Kelly GT, Zhang H, Watanabe CM. Characterization of AziR, a resistance protein of the DNA cross-linking agent azinomycin B. Mol Biosyst. 2011 Sep;7(9):2563–70. doi: 10.1039/c1mb05136a.
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