(3Z,3'Z)-3,3'-(Hydrazine-1,2-diylidene)bis(5-fluoroindolin-2-one) | 1401343-93-8

• 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: (3Z,3'Z)-3,3'-(Hydrazine-1,2-diylidene)bis(5-fluoroindolin-2-one)
• CAS: 1401343-93-8
• 化学式: C₁₆H₈F₂N₄O₂
• 分子量: 326.262
• InChiKey: CVNYVVPSBUSZJR-UHFFFAOYSA-N

物化性质

• 密度：
  1.67±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.06
• 重原子数：
  24.0
• 可旋转键数：
  1.0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  82.92
• 氢给体数：
  2.0
• 氢受体数：
  4.0

文献信息

• Synthesis, in vitro and in vivo antitumor activity of symmetrical bis-Schiff base derivatives of isatin
  作者：Chengyuan Liang、Juan Xia、Dong Lei、Xiang Li、Qizheng Yao、Jing Gao

  DOI：10.1016/j.ejmech.2013.04.040

  日期：2014.3

  synthesized by condensation of the natural or synthetic isatins with hydrazine and were evaluated for their in vitro and in vivo antitumor activities. More than half of the obtained compounds showed potent cytotoxicity according to the MTT assay on five different human cancer cell lines (i.e. HeLa, SGC-7901, HepG2, U251, and A549), with compound 3b 3,3′-(hydrazine-1,2-diylidene)bis (5-methylindolin-2-one)

  通过将天然或合成的靛红与肼缩合，合成了18种对称的靛红双Schiff碱对称衍生物，并对其体外和体内抗肿瘤活性进行了评估。根据MTT分析，获得的化合物中有一半以上对五种不同的人类癌细胞系（即HeLa，SGC-7901，HepG2，U251和A549）显示出有效的细胞毒性，其中化合物3b 3,3'-（hydrazine-1 ，2二亚基）双（5-甲基二氢-2-酮）是对HepG2（IC的最有效的化合物50  〜4.23微米）。还发现3b以40mg / kg的剂量能够基本上抑制荷属HepS的小鼠上的肿瘤生长。H 2中的实时活细胞成像和跟踪B标记的HeLa细胞显示3b可以诱导有丝分裂干扰和凋亡相关的细胞死亡。在机制研究中，3b通过下调cyclin B1和cdc 2的表达而使HepG2细胞的G2 / M期细胞周期停滞。
• Novel N, N'-Hydrazino-bis-isatin Derivatives with Selective Activity Against Multidrug-Resistant Cancer Cells
  申请人：Mohamed Hassan Tarek Aboul-Fadl

  公开号：US20120252860A1

  公开（公告）日：2012-10-04

  The invention is directed to a compound of Formula (I), wherein R is selected from the group consisting of hydrogen atom and unsubstituted or substituted phenyl group; R 1 is selected from the group consisting of hydrogen atom and unsubstituted or substituted phenyl group; X is selected from the group consisting of hydrogen atom or halogen atom; and Y is selected from the group consisting of hydrogen atom, halogen atom, C 1 -C 4 alkyl group, nitro group, and —OCF 3 group, as well as for its use in therapy, preferably for the treatment of cancer, and to a related pharmaceutical composition, the use of the compound for the manufacture of a medicament for the respective medical indication, and a method of synthesis of the compounds of the invention.

  本发明涉及一种式（I）的化合物，其中R选自氢原子和未取代或取代的苯基团组成的群；R1选自氢原子和未取代或取代的苯基团组成的群；X选自氢原子或卤素原子；Y选自氢原子、卤素原子、C1-C4烷基、硝基和—OCF3基团组成的群。该化合物被用于治疗，特别是用于治疗癌症，并且涉及相关的制药组合物、用于制造相应医疗适应症药物的化合物的使用以及制备该化合物的合成方法。
• Novel N,N'-hydrazino-bis-isatin derivatives with selective activity against multidrug-resistant cancer cells
  申请人：King Saud University

  公开号：EP2508512B1

  公开（公告）日：2013-07-31
• US8497296B2
  申请人：——

  公开号：US8497296B2

  公开（公告）日：2013-07-30