phenyl-phosphonic acid monoamide | 57246-28-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: phenyl-phosphonic acid monoamide
• 英文别名: Phenyl-phosphonsaeure-monoamid；dihydroxy-imino-phenyl-λ5-phosphane
• CAS: 57246-28-3
• 化学式: C₆H₈NO₂P
• 分子量: 157.109
• InChiKey: HRQOQAVEPWMWFE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  64.3
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• [EN] PROCESS FOR THE PREPARATION OF IODIDES<br/>[FR] PROCÉDÉ DE PRÉPARATION D'IODURES
  申请人：TECHNION R & D FOUNDATION LTD

  公开号：WO2011154953A1

  公开（公告）日：2011-12-15

  This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.

  这项发明涉及利用N-碘酰胺从相应的羧酸制备高产量的烷基或芳基碘化物的过程。
• PEPTIDE AND PEPTIDE MIMETIC BINDING ANTAGONISTS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE
  申请人：THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH & HUMAN SERVIC

  公开号：US20160039872A1

  公开（公告）日：2016-02-11

  The invention provides novel compounds that may serve as anticancer therapeutics. The compounds of the invention bind to polo-like kinases through the polo-box domain. In certain embodiments, the compounds of the invention are POM-protected peptide derivatives. The use of cationic bis-alkyl his residues in combination with a mono POM-protected pho-phoryl group results in a peptide possessing an overall neutral charge. The peptide derivatives of the invention have achieved both good efficacy and an enhanced bioavailability. The invention also provides methods of use, compositions, and kits thereof. Further, the invention provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.

  该发明提供了可能用作抗癌治疗的新化合物。该发明的化合物通过波洛盒结构结合到波洛样激酶。在某些实施方式中，该发明的化合物是POM保护的肽衍生物。在结合了阳离子双烷基组氨酸残基和单个POM保护的磷酸化基团的情况下，得到的肽具有整体中性电荷。该发明的肽衍生物既具有良好的疗效又具有增强的生物利用度。该发明还提供了使用方法、组合物和相关试剂盒。此外，该发明提供了一种新的设计和/或合成磷酸化肽衍生物的方法，这些衍生物可用作治疗剂。
• Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use
  申请人：Burke, Jr. Terrence R.

  公开号：US10266565B2

  公开（公告）日：2019-04-23

  Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.

  提供了一种新型化合物，通过波洛盒结构结合波洛样激酶。在某些实施例中，这些新型化合物是PEG化肽。根据本发明，这些PEG化肽表现出高PBD结合亲和力。在某些实施例中，这些PEG化肽在整个细胞系统中也表现出活性。本发明还提供了一种通过波洛盒结构结合波洛样激酶且具有降低阴离子电荷的化合物。此外，还提供了PEG化肽的设计和/或合成方法以及使用这些方法。本发明提供了这些化合物的使用方法和合成方法。
• Combination of FBPase inhibitors and antidiabetic agents useful for the treatment of diabetes
  申请人：——

  公开号：US20030073728A1

  公开（公告）日：2003-04-17

  A combination therapy of at least one FBPase inhibitor and at least one other antidiabetic agent is disclosed.

  揭示了至少一种FBPase抑制剂和至少一种其他抗糖尿病药物的联合治疗。
• PEPTIDE MIMETIC LIGANDS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE
  申请人：Burke, JR. Terrence R.

  公开号：US20120065146A1

  公开（公告）日：2012-03-15

  Found in various eukaryotic organisms, polo-like kinases (collectively, Plks) are a conserved subfamily of Ser/Thr protein kinases that play critical roles in cell proliferation. Provided herein are compounds that specifically inhibit the activity of Plks, specifically Plk1. Further provided herein are methods for use of the compounds for the treatment of hyperproliferative disorders, particularly cancer. Also provided are uses of the compounds for the preparation of a medicament.

  在各种真核生物中发现的波罗样激酶（Plks）是一类保守的Ser / Thr蛋白激酶亚家族，它们在细胞增殖中发挥关键作用。本文提供了特异性抑制Plks，特别是Plk1活性的化合物。本文还提供了使用这些化合物治疗高增殖性疾病，特别是癌症的方法。此外，还提供了使用这些化合物制备药物的用途。