WNN1770-D009 | 353484-21-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: WNN1770-D009
• 英文别名: CCX-1959；3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4,8-dicarboxylic acid
• CAS: 353484-21-6
• 化学式: C₁₄H₁₃NO₄
• 分子量: 259.262
• InChiKey: RKSORIGFRQYENG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  86.6
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  WNN1770-D009 、 三甲基硅烷化重氮甲烷 以 甲醇 、 正己烷 为溶剂， 反应 0.17h， 以1.1 mg的产率得到CRS-057
  参考文献：
  名称：

  Discovery and Characterization of Novel Small Molecule Inhibitors of Human Cdc25B Dual Specificity Phosphatase

  摘要：

  Cdc25A 和 Cdc25B 双特异性磷酸酶是细胞周期转换和增殖的关键调节因子。它们具有致癌特性，在许多人类肿瘤中过度表达。由于选择性 Cdc25 磷酸酶抑制剂将成为有价值的生物学工具和可能的治疗药物，我们对体外抑制 Cdc25 的小分子库进行了检测。现在，我们报告发现了两种具有细胞活性、结构不同的新型 Cdc25 抑制剂。环戊喹啉 3a,4,5,9b-四氢-3 H -环戊[c ]喹啉-4,8-二羧酸（5661118）和萘呋二酮 3-苯甲酰基-萘并[1,2-b ]呋喃-4,5-二酮（5169131）对重组 Cdc25 的体外 IC50 值为 2.5 至 11 μM，对其他磷酸酶的抑制作用较弱。与 5661118 不同的是，5169131 可对 Cdc25B 造成可逆抑制，并显示出竞争性抑制动力学。5661118 没有抑制生长的活性，而 10 至 30 μM 的 5169131 会导致 G1/S 和 G2/M 停滞。我们还发现 5169131 可抑制人 PC-3 前列腺癌和 MDA-MB-435 乳腺癌细胞的增殖。在 5169131 处理 1 小时后，细胞周期蛋白依赖性激酶上出现了浓度依赖性 Tyr15 过度磷酸化，这与 Cdc25 抑制作用一致。对DNA拓扑异构酶II抑制剂有抗药性的细胞与亲代细胞一样对5169131敏感，这表明这种醌化合物在体内不会抑制拓扑异构酶II。分子建模被用来预测抑制剂与 Cdc25B 之间的潜在相互作用位点，并为实验观察的分子起源提供见解。根据其动力学特征和细胞活性，我们认为 5169131 是进一步研究 Cdc25 细胞作用的绝佳工具。

  DOI：

  10.1124/mol.104.001784

文献信息

• COSMETIC OR DERMATOLOGICAL COMPOSITION COMPRISING A POLYMER BEARING JUNCTION GROUPS, AND COSMETIC TREATMENT PROCESS
  申请人：Chodorowski-Kimmes Sandrine

  公开号：US20100239509A1

  公开（公告）日：2010-09-23

  The present patent application relates to a cosmetic or dermatological composition comprising, in a cosmetically or dermatologically acceptable medium, a polymer comprising: (a) a polymer backbone that may be obtained by reaction: of a polyol comprising 3 to 6 hydroxyl groups; of a monocarboxylic acid containing 6 to 32 carbon atoms; of a polycarboxylic acid comprising at least two carboxylic groups COOH, and/or of a cyclic anhydride such as a polycarboxylic acid and/or of a lactone comprising at least one carboxylic group COOH; and (b) at least one junction group linked to the said polymer backbone and capable of establishing H bonds with one or more partner junction groups, each pairing of a junction group involving at least three H (hydrogen) bonds. The patent application also concerns a cosmetic treatment process using the said composition.

  本专利申请涉及一种化妆品或皮肤科学组合物，包括在化妆品或皮肤科学上可接受的介质中，包含以下聚合物的组合物：(a) 由以下反应得到的聚合物骨架：含有3至6个羟基的多元醇；含有6至32个碳原子的一元羧酸；至少含有两个羧基COOH的多元羧酸，和/或类似多元羧酸的环酐和/或至少含有一个羧基COOH的内酯；以及(b) 至少一个连接到所述聚合物骨架的连接基团，并能够与一个或多个配对连接基团建立H键，每个连接基团的配对涉及至少三个H（氢）键。该专利申请还涉及使用所述组合物的化妆品处理过程。
• COMPOSITION COMPRISING A POLYCONDENSATE, METHOD OF TREATMENT, POLYCONDENSATE, AND METHOD OF PREPARATION
  申请人：GIUSTINIANI Pascal

  公开号：US20090028807A1

  公开（公告）日：2009-01-29

  The present application relates to a cosmetic or pharmaceutical, in particular lipstick, composition comprising a polycondensate The application also relates to a method of cosmetic treatment using the composition, the polycondensate thus defined and a method of preparing the polycondensate.

  本申请涉及一种化妆品或药用品，特别是口红，包括聚缩酸酯的组合物。该申请还涉及一种使用该组合物进行化妆处理的方法，所述聚缩酸酯的定义以及一种制备聚缩酸酯的方法。
• COSMETIC OR PHARMACEUTICAL COMPOSITION COMPRISING A POLYCONDENSATE, THE SAID POLYCONDENSATE AND METHOD OF COSMETIC TREATMENT
  申请人：Malle Gerard

  公开号：US20100272660A1

  公开（公告）日：2010-10-28

  The present application relates to a cosmetic or pharmaceutical composition comprising a polycondensate capable of being obtained by the reaction of the following monomers alone: of 10 to 30% by weight, relative to the total weight of the polycondensate, of one or more polyols comprising 3 to 6 hydroxyl groups; of 30 to 80% by weight, relative to the total weight of the polycondensate, of one or more linear, branched and/or cyclic, saturated or unsaturated, non-aromatic monocarboxylic acids comprising 6 to 32 carbon atoms; of 1 to 40% by weight, relative to the total weight of the polycondensate, of one or more polycarboxylic acids and/or cyclic anhydrides of such a polycarboxylic acid and/or lactones comprising at least one COOH group; and optionally of 0.1 to 15% by weight, relative to the total weight of the polycondensate, of one or more silicones having a hydroxyl and/or carboxyl functional group. The application also relates to a method of cosmetic treatment using the said composition, and the polycondensate thus defined.

  本申请涉及一种化妆品或药用组合物，包括由以下单体反应而得的聚缩酸酯：相对于聚缩酸酯的总重量，占10至30%的一种或多种含有3至6个羟基的多元醇；占30至80%的一种或多种线性、支链和/或环状、饱和或不饱和、非芳香族的单羧酸，含有6至32个碳原子；占聚缩酸酯总重量的1至40%的一种或多种多羧酸和/或多羧酸的环状酐和/或含有至少一个COOH基团的内酯；以及可选地占聚缩酸酯总重量的0.1至15%的一种或多种硅氧烷，具有羟基和/或羧基官能团。该申请还涉及使用所述组合物进行化妆处理的方法，以及如此定义的聚缩酸酯。
• METHODS AND COMPOSITIONS FOR INHIBITING CNKSR1
  申请人：Phusis Therapeutics Inc.

  公开号：EP2931280B1

  公开（公告）日：2018-02-14
• ANTI-INFLAMMATORY COMPOSITIONS AND METHODS OF USE
  申请人：McMaster Brian

  公开号：US20070072875A1

  公开（公告）日：2007-03-29

  The present invention is directed to pharmaceutical compositions containing active compounds, which inhibit the activity of the chemokines, MIP-1α and RANTES. It also is directed to methods of treating inflammatory and immunoregulatory disorders and diseases using these pharmaceutical compositions.