3-Bromoacetamido-benzoylurea

• 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: 3-Bromoacetamido-benzoylurea
• 英文别名: 3-[(2-bromoacetyl)amino]-N-carbamoylbenzamide
• 化学式: C₁₀H₁₀BrN₃O₃
• 分子量: 300.11
• InChiKey: ROTXPDBINYTRPW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  101
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• Aminobenzoic acid derivatives having anti-tumorigenic activity, methods of making and using the same
  申请人：——

  公开号：US20020022747A1

  公开（公告）日：2002-02-21

  Haloacetoamido, benzoic acid derivatives having anti-tumorigenic activity. Examples of the haloacetoamido, benzoic acid derivatives include 3-chloroacetoamido, benzoylurea, 3-bromoacetoamido, benzoylurea, 3-iodoacetoamido, benzoylurea, ethyl-3-chloroacetoamido, benzoate, ethyl-3-bromoacetoamido, benzoate and ethyl-3-iodoacetoamido, benzoate. Intermediates for synthesizing the derivatives, along with method of making and using the derivatives, are also provided.

  Haloacetoamido，苯甲酸衍生物具有抗肿瘤活性。Haloacetoamido，苯甲酸衍生物的例子包括3-氯乙酰胺，苯甲酰脲，3-溴乙酰胺，苯甲酰脲，3-碘乙酰胺，苯甲酰脲，乙基-3-氯乙酰胺，苯甲酸酯，乙基-3-溴乙酰胺，苯甲酸酯和乙基-3-碘乙酰胺，苯甲酸酯。还提供了合成衍生物的中间体，以及制备和使用衍生物的方法。
• Anti-S-phase tubulin ligands
  申请人：——

  公开号：US20020065229A1

  公开（公告）日：2002-05-30

  It is presently accepted that the mechanism of action for all anti-tumor tubulin ligands involves the perturbation of microtubule dynamics during the G2/M phase of cell division and subsequent entry into apoptosis (1). In this invention, we report a novel tubulin ligands which have a unique mechanism of action. These compounds,. halogenated derivatives of acetamido benzoyl ethyl ester (HAABE), arrest cancer cells in S-phase and cause cell death by a combination of apoptosis (DNA ladder) and necrosis (DNA degradation) type mechanisms. Normal cells are not affected at the same concentrations of compound. The ligands bind covalently to tubulin in vitro and in vivo and shows potent cancericidal activity in tissue culture assays and in animal tumor models. These compounds target early S-phase at the G1/S transition rather than the G2/M phase and mitotic arrest. Bcl-2 phosphorylation, a marker of mitotic microtubule inhibition by other tubulin ligands was dramatically altered, phosphorylation was rapid and biphasic rather than a slow linear event. The halogenated ethyl ester series of derivatives thus constitute a unique set of tubulin ligands which induce a novel mechanism of cancer cell death.

  目前公认，所有抗肿瘤微管蛋白配体的作用机制都是在细胞分裂的 G2/M 阶段扰乱微管动力学，随后进入细胞凋亡阶段（1）。在本发明中，我们报告了一种具有独特作用机制的新型微管蛋白配体。这些化合物，即乙酰氨基苯甲酰乙酯的卤代衍生物（HAABE），可使癌细胞停滞在 S 期，并通过凋亡（DNA 梯形）和坏死（DNA 降解）两种机制导致细胞死亡。相同浓度的化合物不会影响正常细胞。配体在体外和体内与微管蛋白共价结合，在组织培养试验和动物肿瘤模型中显示出强大的杀癌活性。这些化合物针对的是 G1/S 转换的早期 S 期，而不是 G2/M 期和有丝分裂停滞期。Bcl-2 磷酸化是其他微管蛋白配体抑制有丝分裂微管的标志，这些化合物的磷酸化发生了显著变化，磷酸化迅速且呈双相，而不是缓慢的线性磷酸化。因此，卤代乙酯系列衍生物构成了一组独特的微管蛋白配体，可诱导一种新的癌细胞死亡机制。
• Compounds, in particularly of urea derivatives or esters of haloacetamidobenzoic acid and use thereof for the treatment of parasitic diseases
  申请人：Lepape Patrice

  公开号：US20050165068A1

  公开（公告）日：2005-07-28

  The invention relates to the use of a compound of general formula (I) for the production of a medicament used for treating parasitic diseases, particularly leishmaniasis.

  本发明涉及通式（I）化合物用于生产治疗寄生虫病，特别是利什曼病的药物。
• METHOD OF DIAGNOSIS OF PROSTATE CANCER
  申请人：Uropath PTY. Ltd.

  公开号：EP1107665A1

  公开（公告）日：2001-06-20
• EP1107665A4
  申请人：——

  公开号：EP1107665A4

  公开（公告）日：2003-04-02