Benzylsulfonylformic acid | 140894-99-1

• 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: Benzylsulfonylformic acid
• CAS: 140894-99-1
• 化学式: C₈H₈O₄S
• 分子量: 200.215
• InChiKey: ZVRCXMLHCLZLJD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  79.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (E)-3-(3-hydroxy-4-methoxyphenyl)-1-(5-methoxy-2,2-dimethyl-2H-chromen-8-yl)prop-2-en-1-one 、 Benzylsulfonylformic acid 在 4-二甲氨基吡啶 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 反应 12.0h， 以81%的产率得到(E)-2-methoxy-5-(3-(5-methoxy-2,2-dimethyl-2H-chromen-8-yl)-3-oxoprop-1-en-1-yl)phenyl phenylmethanesulfonate
  参考文献：
  名称：

  Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents

  摘要：

  Twenty-five novel pyranochalcone derivatives were synthesized and evaluated for their in vitro and in vivo antiproliferative activities. Among them, compound 10i exhibited superior potent activity against 21 tumor cell lines including multidrug resistant phenotype with the IC50 values ranged from 0.09 to 1.30 mu M. In addition, 10i significantly induced cell cycle arrest in G2/M phase, promoted tubulin polymerization into microtubules and caused microtubule stabilization. Further studies confirmed that 10i significantly suppressed the growth of tumor volume in HepG2 xenograft tumor model. Our study demonstrated that 10i could have beneficial antitumor activity as a novel microtubule stabilizing agent. (C) 2013 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2013.01.007

文献信息

• Base-substituted benzylamine analogs for use as coagulation factor xa inhibitors, the production and use thereof
  申请人：Stürzebecher Jörg

  公开号：US20070066539A1

  公开（公告）日：2007-03-22

  The invention relates to the novel base-substituted benzylamine analogs of general formula (I), wherein A represents P 2 -P 1 with P 1 =(A) and P 2 =(B), for use as coagulation factor Xa inhibitors. The invention also relates to the production and use of said analogs in the therapy and prophylaxis of cardiovascular diseases and thromboembolic events.

  该发明涉及一般式（I）的新型基取代苄胺类似物，其中A代表P2-P1，P1=(A)和P2=(B)，用作凝血因子Xa抑制剂。该发明还涉及所述类似物的制备和在心血管疾病和血栓栓塞事件的治疗和预防中的应用。
• Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung
  申请人：The Medicines Company (Leipzig) GmbH

  公开号：EP2292640A2

  公开（公告）日：2011-03-09

  Neue basisch-substiutierte Benzlaminanaloga der allgemeinen Formel (I) als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung zur Therapie und Prophylaxe von kardiovaskulären Erkrankungen und thromboembolischen Ereignissen.

  作为凝血因子 Xa 抑制剂的通式 (I) 的新型碱性取代苯甲胺类似物、其制备方法以及在治疗和预防心血管疾病和血栓栓塞事件中的应用。
• BASISCH-SUBSTITUIERTE BENZYLAMINANALOGA ALS INHIBITOREN DES GERINNUNGSFAKTORS XA, IHRE HERSTELLUNG UND VERWENDUNG
  申请人：The Medicines Company (Leipzig) GmbH

  公开号：EP1664089B1

  公开（公告）日：2011-11-16
• INTERVERTEBRAL BODY IMPLANT, INSTRUMENT AND METHOD
  申请人：Asaad Wagdy W.

  公开号：US20110264218A1

  公开（公告）日：2011-10-27

  Interbody implant systems and methods of implant interbody implants are described. In one aspect, an implant includes a body have a distal end portion and a proximal end portion and a first articulation surface formed at a distal end of the distal end portion. An insertion instrument includes an elongate shaft having a proximal end portion and a distal end portion; and a second articulation surface formed at a distal end of the distal end portion. The second articulation surface is configured to interface with the first articulation surface. An attachment member is configured to connect the implant to the insertion instrument. The attachment member is actuatable to compress the first and second articulation surfaces together in a locked configuration with sufficient force to prevent relative rotation between the first and second articulation surfaces. The attachment member is actuatable to reduce an amount of compression force existing in the locked configuration to place the first and second articulation surfaces in an unlocked configuration such that the first articulation surface can rotate relative to the second articulation surface.
• US9090658B2
  申请人：——

  公开号：US9090658B2

  公开（公告）日：2015-07-28