cystylpropargylamide

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: cystylpropargylamide
• 英文别名: (2R)-2-amino-N-propyl-3-sulfanylpropanamide
• 化学式: C₆H₁₄N₂OS
• 分子量: 162.256
• InChiKey: FYZXZZKSQWWNRX-YFKPBYRVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  10
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  56.1
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  在 三异丙基硅烷 、 三氟乙酸 作用下， 以 水 为溶剂， 反应 0.5h， 生成 cystylpropargylamide
  参考文献：
  名称：

  [EN] HYBRID IMMUNOGLOBULIN CONTAINING NON-PEPTIDYL LINKAGE
  [FR] IMMUNOGLOBULINE HYBRIDE CONTENANT UNE LIAISON NON PEPTIDIQUE

  摘要：

  公开号：

  WO2014144911A3

文献信息

• Direct amidation of unprotected amino acids using B(OCH₂CF₃)₃
  作者：Rachel M. Lanigan、Valerija Karaluka、Marco T. Sabatini、Pavel Starkov、Matthew Badland、Lee Boulton、Tom D. Sheppard

  DOI：10.1039/c6cc05147b

  日期：——

  A commercially available borate ester, B(OCH2CF3)3, can be used to achieve protecting-group free direct amidation of [small alpha]-amino acids with a range of amines in cyclopentyl methyl ether. The method can...

  可商购的硼酸酯B（OCH 2 CF 3）3可用于在环戊基甲基醚中实现小α-氨基酸与一系列胺的无保护基的直接酰胺化。该方法可以...
• 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：US20140142044A1

  公开（公告）日：2014-05-22

  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. The compounds of the invention have potential therapeutic activity in view of their binding and inhibitory activities towards Plk1. They are based on the amino acid sequence PLHSpT (phosphorylated Thr). The PEG moiety, when present, is covalently attached at the N-terminus. The invention also encompasses derivatives having substituents on the Pro and/or the His side chains, substituents on the phosphate group, the replacement of His with Gln, the replacement of Pro with a N-substituted Gly, the replacement of Ser with Ala, as well as HS-pT fragments with N-terminal alkoxycarbonyl group and PLHS fragments with a C-terminal glyco-imino-alkylxyalkylamide group.

  本发明提供了一种通过Polo-box结构域结合到Polo-like激酶的新化合物。在某些实施例中，这些新化合物是聚乙二醇化肽。根据本发明，这些聚乙二醇化肽表现出高的PBD结合亲和力。在某些实施例中，这些聚乙二醇化肽还在整个细胞系统中表现出活性。本发明还提供了通过Polo-box结构域结合到Polo-like激酶并具有降低阴离子电荷的化合物。进一步提供了设计和/或合成这些聚乙二醇化肽的方法以及使用它们的方法。本发明提供了这些化合物的使用方法和合成方法。这些化合物由氨基酸序列PLHSpT（磷酸化苏氨酸）构成。当存在PEG基团时，PEG基团以共价键连接在N-末端。本发明还包括具有Pro和/或His侧链置换基团、磷酸酯基团置换基团、His被Gln置换、Pro被N-取代Gly置换、Ser被Ala置换的衍生物，以及具有N-末端烷氧羰基基团的HS-pT片段和具有C-末端糖基亚氨基烷氧基烷酰胺基团的PLHS片段。
• [EN] METHOD FOR USING CFH OR APOH AS A BIOCHEMICAL MARKER FOR DIAGNOSIS OF ACUTE MYELOID LEUKEMIA<br/>[FR] PROCÉDÉ POUR UTILISER CFH OU APOH EN TANT QUE MARQUEUR BIOCHIMIQUE POUR LE DIAGNOSTIC DE LA LEUCÉMIE MYÉLOÏDE AIGUË
  申请人：LEE SEUNG WON

  公开号：WO2010123216A2

  公开（公告）日：2010-10-28

  본 발명은 급성골수성백혈병의 관해 진단방법에 관한 것으로, 보다 구체적으로는 환자의 혈청에 포함된 CFH (complement factor H) 또는 ApoH (apolipoprotein H)를 급성골수성백혈병의 관해 진단용 생화학적 마커로 사용하는 방법에 관한 것이다. 본 발명의 방법에 의하면 급성골수성백혈병 치료시 사람 몸의 반응에 대한 생물학적 메카니즘을 확인하기 위한 새로운 생화학적 마커를 제공할 뿐만 아니라, 상기 생화학적 마커의 농도를 통해 질병 예후가 좋거나 좋지 않은지 정확하게 진단할 수 있는 우수한 효과가 있다.
• [EN] PEPTIDE AND PEPTIDE MIMETIC BINDING ANTAGONISTS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE<br/>[FR] ANTAGONISTES DE LIAISON PEPTIDIQUE ET MIMÉTIQUE DE PEPTIDE DE DOMAINE POLO BOX DOMAIN DE KINASE 1 DE TYPE POLO ET MÉTHODES D'UTILISATION
  申请人：US HEALTH

  公开号：WO2014153101A2

  公开（公告）日：2014-09-25

  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 phophoryl 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.