Boc-(4-amino-3-iodo)-D-Phe-OH | 846569-62-8

• 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: Boc-(4-amino-3-iodo)-D-Phe-OH
• 英文别名: (2R)-3-(4-amino-3-iodophenyl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoic acid
• CAS: 846569-62-8
• 化学式: C₁₄H₁₉IN₂O₄
• 分子量: 406.22
• InChiKey: XCLBYJSMRUIHMO-LLVKDONJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  21
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  102
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  Boc-4-氨基-D-苯丙氨酸 在 N-碘代丁二酰亚胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以2.14 g的产率得到Boc-(4-amino-3-iodo)-D-Phe-OH
  参考文献：
  名称：

  HALOGENATED SOMATOSTATIN ANALOGS WITH MULTIPLE SOMATOSTATIN RECEPTOR SUBTYPE SELECTIVITY

  摘要：

  The present invention relates to halogenated somatostatin analogs with selectivity for multiple somatostatin receptor subtypes and pharmaceutical compositions comprising the same. Moreover, the present invention relates to said halogenated somatostatin analogs and pharmaceutical compositions for use in therapy and/or diagnosis, for example in the treatment and/or diagnosis of diseases (e.g., cancer such as a neuroendocrine cancer) that are characterized by a high expression (e.g., overexpression) of one or more somatostatin receptor subtypes (e.g., somatostatin receptor 2 (SST2) and/or somatostatin receptor 5 (SST5)).

  公开号：

  WO2024047112A1

文献信息

• [EN] SOMATOSTATIN ANALOGS WITH INHIBITORY ACTIVITY TO GROWTH HORMONE RELEASE<br/>[FR] ANALOGUES DE SOMATOSTATINE A ACTIVITE INHIBITRICE DE LIBERATION D'HORMONE DE CROISSANCE
  申请人：UNIV CALIFORNIA

  公开号：WO2005018682A3

  公开（公告）日：2005-04-28
• Discovery of Iodinated Somatostatin Analogues Selective for hsst2 and hsst5 with Excellent Inhibition of Growth Hormone and Prolactin Release from Rat Pituitary Cells
  作者：Sandra Blaj Moore、Joost van der Hoek、Antonia de Capua、Peter M. van Koetsveld、Leo J. Hofland、Steven W. J. Lamberts、Murray Goodman

  DOI：10.1021/jm050376t

  日期：2005.10.1

  Inhibition of growth hormone (GH) and prolactin (PRL) release from the anterior pituitary gland is mediated through somatostatin receptor subtypes sst2 and sst5. It has been found that somatostatin (SS) analogues that are selective for both receptor subtypes are more effective at inhibiting GH and PRL release than monospecific analogues alone. We synthesized several disulfide-bridged octapeptide SS analogues. Iodinated compounds 7, (4-amino-3-iodo)-D-Phe-c[Cys-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH2, and 9,(4-amino-3-iodo)-D-Phe-c[Cys-(3-iodo)-Tyr-D-Trp-Lys-Val-Cys]-Thr-NH2, were as potent as somatostatin in binding at receptors hsst2 and hsst5 and inhibited GH and PRL release from rat pituitary cells as potently as somatostatin.
• Somatostatin analogs with inhibitory activity to growth hormone release
  申请人：Goodman Murray

  公开号：US20070041902A1

  公开（公告）日：2007-02-22

  Provided are therapeutic and diagnostic somatostatin analogs including radiotherapeutic and radiodiagnostic Reagents, and methods of making and use thereof.
• SOMATOSTATIN ANALOGS WITH INHIBITORY ACTIVITY TO GROWTH HORMONE RELEASE
  申请人：Goodman Murray

  公开号：US20110243845A1

  公开（公告）日：2011-10-06

  Provided are therapeutic and diagnostic somatostatin analogs including radiotherapeutic and radiodiagnostic reagents, and methods of making and use thereof.
• US7968080B2
  申请人：——

  公开号：US7968080B2

  公开（公告）日：2011-06-28