N-(2,6-dioxo-1-phenacylpiperidin-3-yl)acetamide

• 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: N-(2,6-dioxo-1-phenacylpiperidin-3-yl)acetamide
• 化学式: C₁₅H₁₆N₂O₄
• 分子量: 288.3
• InChiKey: ZOUDJLOPMJRMCU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  83.6
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] CATIONIC LIPID CORDIARIMIDE HYBRID COMPOUNDS AND A PROCESS FOR PREPARATION THEREOF<br/>[FR] COMPOSÉS HYBRIDES LIPIDE CATIONIQUE-CORDIARIMIDE ET LEUR PROCÉDÉ DE PRÉPARATION
  申请人：COUNCIL SCIENT IND RES

  公开号：WO2015189856A1

  公开（公告）日：2015-12-17

  The present invention relates to the cationic lipid cordiaroimide hybrid compounds of formula I. The present invention provides a process for preparation of these compounds is also being elaborated. The compounds described provides anticancerous activity against cell lines including PC-3 (prostate cancer), HepG2 (liver cancer), MCF-7 (breast cancer) and NIH/3T3 (non cancer) cells. The compound was also capable of inducing caspase-3 mediated apoptosis in HepG2 cells by arresting the cell cycle in the G1 phase. Furthermore, the compound exhibited DNA ligase I inhibition. The present class of cationic lipid cordiarimide hybrids is likely to find specific use in developing novel targeted therapies for liver and prostate cancers.

  本发明涉及公式I的阳离子脂质cordiaroimide混合物化合物。本发明提供了一种制备这些化合物的方法。所描述的化合物对包括PC-3（前列腺癌）、HepG2（肝癌）、MCF-7（乳腺癌）和NIH/3T3（非癌症）细胞在内的细胞系具有抗癌活性。该化合物还能够通过在G1期阻止细胞周期来诱导HepG2细胞中的caspase-3介导的凋亡。此外，该化合物表现出DNA连接酶I的抑制作用。目前这类阳离子脂质cordiarimide混合物可能在开发针对肝癌和前列腺癌的新型靶向治疗中找到特定用途。
• Cationic lipid cordiarimide hybrid compounds and a process for preparation thereof
  申请人：COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH

  公开号：US10266564B2

  公开（公告）日：2019-04-23

  The present invention relates to the cationic lipid cordiaroimide hybrid compounds of formula I. The present invention provides a process for preparation of these compounds is also being elaborated. The compounds described provides anticancerous activity against cell lines including PC-3 (prostate cancer), HepG2 (liver cancer), MCF-7 (breast cancer) and NIH-1/3T3 (non cancer cells. The compound was also capable of inducing caspase-3 mediated apoptosis in HepG2 cells by arresting the cell cycle in the G1 phase. Furthermore, the compound exhibited DNA ligase I inhibition. The present class of cationic lipid cordiarimide hybrids is likely to find specific use in developing novel targeted therapies for liver and prostate cancers.

  本发明涉及式 I 的阳离子脂质堇酰亚胺杂化化合物。本发明还提供了制备这些化合物的工艺。所述化合物对包括 PC-3（前列腺癌）、HepG2（肝癌）、MCF-7（乳腺癌）和 NIH-1/3T3（非癌细胞）在内的细胞系具有抗癌活性。该化合物还能使细胞周期停滞在 G1 期，从而诱导 HepG2 细胞中由 Caspase-3 介导的凋亡。此外，该化合物还具有 DNA 连接酶 I 抑制作用。本类阳离子脂质堇青霉酰胺混合物可能会在开发治疗肝癌和前列腺癌的新型靶向疗法中找到特殊用途。
• CATIONIC LIPID CORDIARIMIDE HYBRID COMPOUNDS AND A PROCESS FOR PREPARATION THEREOF
  申请人：COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH

  公开号：US20170137462A1

  公开（公告）日：2017-05-18

  The present invention relates to the cationic lipid cordiaroimide hybrid compounds of formula I. The present invention provides a process for preparation of these compounds is also being elaborated. The compounds described provides anticancerous activity against cell lines including PC-3 (prostate cancer), HepG2 (liver cancer), MCF-7 (breast cancer) and NIH-1/3T3 (non cancer cells. The compound was also capable of inducing caspase-3 mediated apoptosis in HepG2 cells by arresting the cell cycle in the G1 phase. Furthermore, the compound exhibited DNA ligase I inhibition. The present class of cationic lipid cordiarimide hybrids is likely to find specific use in developing novel targeted therapies for liver and prostate cancers.