1,1-Bis-(4-hydroxy)-phenyl-2-phenyl-2-chloro-ethylene | 106692-29-9

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: 1,1-Bis-(4-hydroxy)-phenyl-2-phenyl-2-chloro-ethylene
• 英文别名: 4-[2-Chloro-1-(4-hydroxyphenyl)-2-phenylethenyl]phenol
• CAS: 106692-29-9
• 化学式: C₂₀H₁₅ClO₂
• 分子量: 322.791
• InChiKey: GPRKJRWPCMWKLE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.8
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  40.5
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  1,1-bis-(4-methoxy)phenyl-2-phenyl-2-chloro-ethylene 生成 1,1-Bis-(4-hydroxy)-phenyl-2-phenyl-2-chloro-ethylene
  参考文献：
  名称：

  Method of using triaryl-ethylene derivatives in the treatment and

  摘要：

  本发明涉及一种在治疗或预防骨组织流失或骨质疏松症中使用三芳基乙烯衍生物的方法。

  公开号：

  US05691384A1

文献信息

• Triaryl-ethylene derivatives
  申请人：Merrell Dow Pharmaceuticals Inc.

  公开号：US05525633A1

  公开（公告）日：1996-06-11

  The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents.

  本发明涉及一种新型三芳基乙烯衍生物，可用作抗肿瘤药物、抗动脉粥样硬化药物和降低胆固醇药物。
• [EN] METHOD OF USING TRIARYL-ETHYLENE DERIVATIVES IN THE TREATMENT AND PREVENTION OF OSTEOPOROSIS<br/>[FR] MODE D'EMPLOI DE DERIVES DU TRIARYL-ETHYLENE POUR LE TRAITEMENT ET LA PREVENTION DE L'OSTEOPOROSE
  申请人：HOECHST MARION ROUSSEL, INC.

  公开号：WO1996016646A1

  公开（公告）日：1996-06-06

  (EN) The present invention relates to a method of using triaryl-ethylene derivatives in the treatment or prevention of bone tissue loss or osteoporosis.(FR) Mode d'emploi de dérivés du triaryl-éthylène pour le traitement et la prévention de la raréfaction du tissu osseux ou ostéoporose.

  该发明涉及使用三芳基乙烯衍生物治疗或预防骨组织流失或骨质疏松的方法。
• Synthesis and estrogen receptor selectivity of 1,1-bis(4-hydroxyphenyl)-2-(p-halophenyl)ethylenes
  作者：Peter C. Ruenitz、Jerome R. Bagley、Nitin T. Nanavati

  DOI：10.1021/jm00402a037

  日期：1988.7

  A series of triarylethylenes (1a-e) were synthesized and evaluated for their ability to compete with [3H]estradiol for high-affinity estrogen receptors (ER) in immature rat uterine cytosol. All compounds showed affinity comparable to that of estradiol, with 1c having the highest affinity and the lowest calculated nonspecific binding of the para-halogenated members. Compound 1a had a higher affinity than did its chlorovinyl counterpart 1b, indicating that a vinyl hydrogen was suitable for high ER affinity in this series. Compound 1c was labeled with 3H ortho to one or both of its hydroxyls. Its ratio of specific to nonspecific binding in rat uterine cytosol, 3.2, was 140% of that of a related triarylethylene, 4-hydroxytamoxifen, and was 24% that of estradiol. Administration of [3H]-1c to immature female rats resulted in accumulation of 3H in uterine tissue which was decreased 39% when [3H]-1c was coadministered with estradiol. The major site of accumulation 1, 4, and 8 h after administration was in the intestinal tract. Chromatographic analysis showed that levels of 1c were less than those of 1c glucuronide in blood plasma, liver, and intestinal contents of rats 1 h after administration of 1c. Uterine 3H was comprised of 85% of 1c and 11% of 1c glucuronide. These results indicate that 1c undergoes ER-mediated uptake in the immature female rat, but selectivity is reduced due to nonspecific accumulation of free and conjugated 1c in uterine tissue.
• RUENITZ, PETER C.;BAGLEY, JEROME R.;NANAVATI, NITIN T., J. MED. CHEM., 31,(1988) N 7, 1471-1475
  作者：RUENITZ, PETER C.、BAGLEY, JEROME R.、NANAVATI, NITIN T.

  DOI：——

  日期：——
• TRIARYL-ETHYLENE DERIVATIVES FOR USE IN THERAPY
  申请人：MERRELL PHARMACEUTICALS INC.

  公开号：EP0720597A1

  公开（公告）日：1996-07-10