(E)-2,4-dichlorostyryl phenyl sulfone | 108476-27-3

• 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: (E)-2,4-dichlorostyryl phenyl sulfone
• 英文别名: (2,4-dichloro-trans-styryl)-phenyl sulfone；(2,4-Dichlor-trans-styryl)-phenyl-sulfon；E-2,4-dichlorostyryl phenyl sulfone；1-[(E)-2-(benzenesulfonyl)ethenyl]-2,4-dichlorobenzene
• CAS: 108476-27-3
• 化学式: C₁₄H₁₀Cl₂O₂S
• 分子量: 313.204
• InChiKey: QPMFUCLWWAQPBD-CMDGGOBGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  42.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  (苯磺酰)乙酸 、 2,4-二氯苯甲醛 以The title compound was obtained in 60-65% yield的产率得到(E)-2,4-dichlorostyryl phenyl sulfone
  参考文献：
  名称：

  Method for protecting normal cells from cytotoxicity of chemotherapeutic agents

  摘要：

  预处理使用α，β不饱和芳基磺酮可以保护正常细胞免受两类抗癌化疗药物的细胞毒副作用。在使用有丝分裂期细胞周期抑制剂或拓扑异构酶抑制剂的抗癌化疗前向患者给予细胞保护性磺酮化合物，可以减少或消除抗癌药物对正常细胞的细胞毒副作用。α，β不饱和芳基磺酮的细胞保护作用使临床医生可以安全地增加抗癌化疗药物的剂量。

  公开号：

  US20040214903A1

文献信息

• (E)-4-carboxystyrl-4-chlorobenzyl sulfone and pharmaceutical compositions thereof
  申请人：——

  公开号：US20030149109A1

  公开（公告）日：2003-08-07

  Pre-treatment with &agr;,&bgr; unsaturated aryl sulfones protects normal cells from the cytotoxic side effects of two classes of anticancer chemotherapeutics. Administration of a cytoprotective sulfone compound to a patient prior to anticancer chemotherapy with a mitotic phase cell cycle inhibitor or topoisomerase inhibitor reduces or eliminates the cytotoxic side effects of the anticancer agent on normal cells. The cytoprotective effect of the &agr;,&bgr; unsaturated aryl sulfone allows the clinician to safely increasing the dosage of the anticancer chemotherapeutic.

  使用α,β-不饱和芳基磺酮进行预处理可以保护正常细胞免受两类抗癌化疗药物的细胞毒副作用。在患者进行含细胞周期有丝分裂期抑制剂或拓扑异构酶抑制剂的抗癌化疗之前，给予一种细胞保护性磺酮化合物，可以减少或消除抗癌药物对正常细胞的细胞毒副作用。α,β-不饱和芳基磺酮的细胞保护作用使得临床医生可以安全地增加抗癌化疗药物的剂量。
• Styryl sulfone anticancer agents
  申请人：——

  公开号：US20020022666A1

  公开（公告）日：2002-02-21

  Styryl sulfone compounds of the invention selectively inhibit proliferation of tumor cells, and induce apoptosis of tumor cells, while sparing normal cells. The compounds, which are useful in the treatment of cancer and other proliferative disorders, have (a) the formula II: 1 wherein n is zero or one; R 1 is selected from the group consisting of hydrogen, chlorine, fluorine and bromine; R 2 is selected from the group consisting of hydrogen, chlorine, fluorine, bromine, methyl and methoxy; and R 3 is selected from the group consisting of hydrogen, chlorine and fluorine; provided, R 2 may not be methyl or methoxy when R 1 and R 3 are both hydrogen and n is zero or one; and R 1 , R 2 and R 3 may not all be hydrogen when n is one; (b) the formula III: 2 wherein R 1 is selected from the group consisting of hydrogen, chlorine, fluorine and bromine; or (c) or the formula IV: 3 wherein R 1 is selected from the group consisting of fluorine and bromine, and R 2 is selected from the group consisting of 2-chlorophenyl, 4-chlorophenyl, 4-fluorophenyl and 2-nitrophenyl.

  本发明的苯乙烯基磺酰化合物选择性地抑制肿瘤细胞的增殖，并诱导肿瘤细胞凋亡，同时不损害正常细胞。这些化合物在治疗癌症和其他增殖性疾病中很有用，具有以下特征： (a) 公式II： 1 其中 n 是零或一； R 1 选自氢、氯、氟和溴的组； R 2 选自氢、氯、氟、溴、甲基和甲氧基的组；和 R 3 选自氢、氯和氟的组；前提是， 当 R 1 和 R 3 都是氢且 n 是零或一时，R 2 不能是甲基或甲氧基；且 当 n 是一时，R 1 、R 2 和 R 3 不能都是氢； (b) 公式III： 2 其中 R 1 选自氢、氯、氟和溴的组；或 (c) 公式IV： 3 其中 R 1 选自氟和溴的组，R 2 选自2-氯苯基、4-氯苯基、4-氟苯基和2-硝基苯基的组。
• [EN] PYRROLE BASED INHIBITORS OF GLYCOGEN SYNTHASE KINASE 3<br/>[FR] INHIBITEURS DE LA GLYCOGENE SYNTHASE KINASE 3 A BASE DE PYRROLE
  申请人：CHIRON CORP

  公开号：WO2004018455A1

  公开（公告）日：2004-03-04

  New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

  提供了基于新吡咯烷基化合物的方法、组合物以及抑制体外糖原合成酶激酶（GSK3）活性和治疗体内GSK3介导的疾病的方法。该发明的方法、化合物和组合物可单独使用，也可与其他药理活性剂结合在一起，用于治疗由GSK3活性介导的疾病，如糖尿病、阿尔茨海默病和其他神经退行性疾病、肥胖、动脉粥样硬化心血管疾病、原发性高血压、多囊卵巢综合征、X综合征、缺血、创伤性脑损伤、躁狂抑郁症、免疫功能缺陷或癌症。
• Method for protecting normal cells from cytotoxicity of chemotherapeutic agents
  申请人：——

  公开号：US20040214903A1

  公开（公告）日：2004-10-28

  Pre-treatment with &agr;,&bgr; unsaturated aryl sulfones protects normal cells from the cytotoxic side effects of two classes of anticancer chemotherapeutics. Administration of a cytoprotective sulfone compound to a patient prior to anticancer chemotherapy with a mitotic phase cell cycle inhibitor or topoisomerase inhibitor reduces or eliminates the cytotoxic side effects of the anticancer agent on normal cells. The cytoprotective effect of the &agr;,&bgr; unsaturated aryl sulfone allows the clinician to safely increasing the dosage of the anticancer chemotherapeutic.

  预处理使用α，β不饱和芳基磺酮可以保护正常细胞免受两类抗癌化疗药物的细胞毒副作用。在使用有丝分裂期细胞周期抑制剂或拓扑异构酶抑制剂的抗癌化疗前向患者给予细胞保护性磺酮化合物，可以减少或消除抗癌药物对正常细胞的细胞毒副作用。α，β不饱和芳基磺酮的细胞保护作用使临床医生可以安全地增加抗癌化疗药物的剂量。
• Formulations of radioprotective alpha, beta unsaturated aryl sulfones
  申请人：Onconova Therapeutics, Inc.

  公开号：EP2769719A1

  公开（公告）日：2014-08-27

  Solution and suspension formulations are provided for administration prior to or after exposure to ionizing radiation for reducing toxic effects of the radiation in a subject which comprises an effective amount of at least one radioprotective α, β unsaturated aryl sulfone wherein the composition has a pH within the range of about 8 to about 9.

  本发明提供了溶液和悬浮液制剂，用于在电离辐射照射前或照射后给药，以减少辐射对受试者的毒性影响，该制剂包含有效量的至少一种辐射保护性 α、β 不饱和芳基砜，其中组合物的 pH 值在约 8 到约 9 的范围内。